Saturated azacyclopropane compounds. They include compounds with substitutions on CARBON or NITROGEN atoms.
Acyclic branched or unbranched hydrocarbons having two carbon-carbon double bonds.
Unsaturated azacyclopropane compounds that are three-membered heterocycles of a nitrogen and two carbon atoms.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)
Any chemical species which acts as an electron-pair donor in a chemical bonding reaction with a LEWIS ACID.
Organic compounds that contain silicon as an integral part of the molecule.
Inorganic compounds that contain bromine as an integral part of the molecule.
Naphthalene derivatives carrying one or more hydroxyl (-OH) groups at any ring position. They are often used in dyes and pigments, as antioxidants for rubber, fats, and oils, as insecticides, in pharmaceuticals, and in numerous other applications.
Communication between animals involving the giving off by one individual of some chemical or physical signal, that, on being received by another, influences its behavior.
A carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries.
Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.
A family of fused-ring hydrocarbons isolated from coal tar that act as intermediates in various chemical reactions and are used in the production of coumarone-indene resins.
A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
The study of the chemical and physical phenomena of radioactive substances.
A pyrano-acridone alkaloid found in RUTACEAE plants.
A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.
A chlorinated epoxy compound used as an industrial solvent. It is a strong skin irritant and carcinogen.
7-Hydroxycoumarins. Substances present in many plants, especially umbelliferae. Umbelliferones are used in sunscreen preparations and may be mutagenic. Their derivatives are used in liver therapy, as reagents, plant growth factors, sunscreens, insecticides, parasiticides, choleretics, spasmolytics, etc.
The study of the structure, preparation, properties, and reactions of carbon compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A gas that condenses under slight pressure. Because of its low boiling point ethyl chloride sprayed on skin produces an intense cold by evaporation. Cold blocks nerve conduction. Ethyl chloride has been used in surgery but is primarily used to relieve local pain in sports medicine.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
Isomeric forms and derivatives of PROPANOL (C3H7OH).
A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms.
Ketonic amines prepared from the condensation of a ketone with formaldehyde and ammonia or a primary or secondary amine. A Mannich base can act as the equivalent of an alpha,beta unsaturated ketone in synthesis or can be reduced to form physiologically active amino alcohols.
The conformation, properties, reaction processes, and the properties of the reactions of carbon compounds.
Inorganic compounds that contain fluorine as an integral part of the molecule.
Aliphatic acids that contain four carbons in a branched-chain configuration. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the 2-carboxypropane structure.

Assaying potential carcinogens with Drosophila. (1/274)

Drosophila offers many advantages for the detection of mutagenic activity of carcinogenic agents. It provides the quickest assay system for detecting mutations in animals today. Its generation time is short, and Drosophila is cheap and easy to breed in large numbers. The simple genetic testing methods give unequivocal answers about the whole spectrum of relevant genetic damage. A comparison of the detection capacity of assays sampling different kinds of genetic damage revealed that various substances are highly effective in inducing mutations but do not produce chromosome breakage effects at all, or only at much higher concentrations than those required for mutation induction. Of the different assay systems available, the classical sex-linked recessive lethal test deserves priority, in view of its superior capacity to detect mutagens. Of practical importance is also its high sensitivity, because a large number of loci in one fifth of the genome is tested for newly induced forward mutations, including small deletions. The recent findings that Drosophila is capable of carrying out the same metabolic activation reactions as the mammalian liver makes the organism eminently suitable for verifying results obtained in prescreening with fast microbial assay systems. An additional advantage in this respect is the capacity of Drosophila for detecting short-lived activation products, because intracellular metabolic activation appears to occur within the spermatids and spermatocytes.  (+info)

Inhibition of DNA replicon initiation by 4-nitroquinoline 1-oxide, adriamycin, and ethyleneimine. (2/274)

The effects of three widely differing chemical carcinogens, 4-nitroquinoline 1-oxide, Adriamycin, and ethyleneimine, on DNA replication were studied by pulse labeling of DNA with [3H]thymidine and sedimentation analysis with alkaline sucrose gradients. At doses that reduced the rate of DNA synthesis to 30 to 60% of control values, only ethyleneimine produced damage that resulted in lower molecular weights of parental DNA. All three chemicals inhibited replicon initiation, but to differing extents. Inhibition of replicon initiation was the first clearly identified effect of 4-nitroquinoline 1-oxide and was the main cause of inhibition of DNA synthesis. Ethyleneimine caused severe inhibition of replicon initiation, but blocks to chain elongation also contributed significantly to the inhibition of overall DNA synthesis. Adriamycin affected replicon initiation to a small but significant extent; the primary cause of inhibition of DNA synthesis by this drug was a slowing of the rate of chain elongation. These results indicate that inhibition of replicon initiation is an important mechanism for the action of DNA-damaging agents in mammalian cells and strengthen the concept that control of DNA replication depends on the structural integrity of a chromosomal subunit that consists of several replicons.  (+info)

Virus directed enzyme prodrug therapy for ovarian and pancreatic cancer using retrovirally delivered E. coli nitroreductase and CB1954. (3/274)

Expression of the E. coli enzyme nitroreductase (NTR) in tumour cells enables them to activate the prodrug CB1954 (5-(aziridin-1-yl)-2,4-dinitrobenzamide), leading to interstrand DNA crosslinking and cell death. Using transfected or retrovirally transduced SKOV3 ovarian carcinoma cell clones, we show a strong correlation between sensitivity to CB1954 and level of NTR enzyme activity. Importantly for clinical application in ovarian cancer, a cisplatin-resistant ovarian tumour cell line remains as susceptible to the NTR-dependent cytotoxicity of CB1954 as parental cells. In mixed populations of NTR-expressing and non-expressing cells, we observe a marked 'bystander killing' effect with this system. The use of NTR-encoding retroviruses from clonal producer cell lines at titres of 5 x 10(5) c.f.u./ml to transduce either established or low passage primary ovarian carcinoma lines only achieves an average 10-fold sensitisation of the cultures at gene transfer efficiencies of 15-25%. Concentration of the retrovirus to 3 x 10(7) c.f.u./ml elevates gene transfer to 80-90% in a single exposure to target cells, resulting in up to 500-fold sensitisation of the entire, unselected SKOV3 population to CB1954. In an initial investigation of NTR/CB1954 for the treatment of tumours in vivo, we observe regression of tumours expressing NTR following administration of CB1954, resulting in significantly increased median survival.  (+info)

Spermine inhibition of the 2,5-diaziridinyl-1,4-benzoquinone (DZQ) crosslinking reaction with DNA duplexes containing poly(purine). poly(pyrimidine) tracts. (4/274)

Upon reduction, 2,5-diaziridinyl-1,4-benzoquinone (DZQ) can form an interstrand guanine to guanine crosslink with DNA duplexes containing a d(GC).d(GC) dinucleotide step. The reaction is enhanced by a thymine positioned 5[prime] to each guanine [i.e. in a d(TGCA). d(TGCA) duplex fragment]. Here we show that spermine can inhibit DZQ crosslink formation in duplexes of sequence d[C(N6)TGCA(M6)C]. d[G(M[prime]6)TG-CA(N[prime]6)G]. For N6= M6= GGGGGG, N6= M6= a 'random' sequence and N6= GGGGGG and M6= a 'random' sequence, spermine concentrations of 20, 1 and 3 microM, respectively, were required for 50% inhibition of the DZQ crosslink. This suggests that spermine is more strongly bound to the polyguanosine tract than the random sequence, making it less available for crosslink inhibition. When the polyguanosine tract is interrupted by N 7-deazaguanine (D) located three bases, d(CGGGDGGTGCAGGDGGGC), and four bases, d(CG-GDGGGTGCAGGGDGGC), from the d(TGCA).d(TGCA) site, 30 and 3 microM spermine, respectively, were required for 50% crosslink inhibition. We suggest that this difference is due to the relative proximity of the three-guanosine tract to the d(TGCA).d(TGCA) site. We were able to confirm these conclusions with further experiments using duplexes containing three-guanosine and two-guanosine tracts and from computer simulations of the spermine-DNA complexes.  (+info)

Occupational asthma and contact dermatitis in a spray painter after introduction of an aziridine cross-linker. (5/274)

A 23-year-old spray painter developed contact dermatitis and respiratory difficulty characterized by small airways obstruction shortly after the polyfunctional aziridine cross-linker CX-100 began to be used in his workplace as a paint activator. The symptoms resolved after he was removed from the workplace and was treated with inhaled and topical steroids. Painters may have an increased risk of asthma due to exposure to a variety of agents, such as isocyanates, alkyd resins, and chromates. This case illustrates the importance of using appropriate work practices and personal protective equipment to minimize exposure. Occupational asthma is diagnosed by a history of work-related symptoms and exposure to known causative agents. The diagnosis is confirmed by serial pulmonary function testing or inhalational challenge testing. The risk of asthma attributable to occupational exposures is probably underappreciated due to underreporting and to inappropriate use of narrow definitions of exposure in epidemiologic studies of attributable risk.  (+info)

Molecular characterization of binding of substrates and inhibitors to DT-diaphorase: combined approach involving site-directed mutagenesis, inhibitor-binding analysis, and computer modeling. (6/274)

The molecular basis of the interaction of DT-diaphorase with a cytotoxic nitrobenzamide CB1954 [5-(aziridin-1-yl)-2, 4-dinitrobenzamide] and five inhibitors was investigated with wild-type DT-diaphorase (human and rat) and five mutants [three rat mutants (rY128D, rG150V, rH194D) and two human mutants (hY155F, hH161Q)]. hY155F and hH161Q were generated to evaluate a hypothesis that Tyr155 and His161 participate in the obligatory two-electron transfer reaction of the enzyme. The catalytic properties of hY155F and hH161Q were compared with a naturally occurring mutant, hP187S. Pro187 to Ser mutation disturbs the structure of the central parallel beta-sheet, resulting in a reduction of the binding affinity of the flavin-adenine dinucleotide prosthetic group. With NADH as the electron donor and menadione as the electron acceptor, the k(cat) values for the wild-type human DT-diaphorase, hY155F, hH161Q, and hP187S were measured as 66 +/- 1, 23 +/- 0, 5 +/- 0 and 8 +/- 2 x 10(3) min(-1), respectively. Because hY155F still has significant catalytic activity, the hydroxyl group on Tyr155 may not be as important as proposed. Interestingly, hY155F was found to be 3. 3 times more active than the human wild-type DT-diaphorase in the reduction of CB1954. Computer modeling based on our results suggests that CB1954 is situated in the active site, with the aziridinyl group pointing toward Tyr155 and the amide group placed near a hydrophobic pocket next to Tyr128. Dicoumarol, Cibacron blue, chrysin, 7,8-dihydroxyflavone, and phenindone are competitive inhibitors of the enzyme with respect to nicotinamide coenzymes. The binding orientations of dicoumarol, flavones, and phenindone in the active site of DT-diaphorase were predicted by results from our inhibitor-binding studies and computer modeling based on published X-ray structures. Our studies generated results that explain why dicoumarol is a potent inhibitor and binds differently from flavones and phenindone in the active site of DT-diaphorase.  (+info)

Effects of aluminum potassium sulfate on learning, memory, and cholinergic system in mice. (7/274)

AIM: To study the relationship between aluminum potassium sulfate (APS) and memory deficits of mice. METHODS: 30, 60, or 90 d after the mice were given daily APS i.g., the step-through latency (STL) was determined with a passive avoidance task. Aluminum (Al) contents in brain and blood were assayed with atomic absorption spectrophotometry. Acetylcholine (ACh) content in brain was determined with chemiluminescent method and choline acetyltransferase (ChAT) activity was measured radiochemically. RESULTS: APS 1 g.kg-1 increased blood-Al only after 30 d. After 60 d, STL, ACh content and ChAT activity decreased by 46.4%, 8.5%, and 22.6%, respectively. These parameters decreased by 50%, 11.1%, and 27.8%, respectively, with increased Al in blood and brain, after 90 d. APS 0.25 g.kg-1 had no effects on mice except blood-Al. In ethylcholine mustard aziridium chloride (AF64A) treated mice, APS 1 g.kg-1 only increased blood and brain-Al. CONCLUSION: The intake of APS 1 g.kg-1.d-1 for 60 d induced learning and memory deficits in mice.  (+info)

Nitroreductase-mediated cell ablation is very rapid and mediated by a p53-independent apoptotic pathway. (8/274)

Nitroreductase (NTR)-mediated selective cell ablation using the prodrug CB1954 has been achieved in vivo by targeting the nitroreductase gene to the luminal cells of the mammary gland in transgenic mice. We report that the cell ablation occurs very rapidly, starting as early as 7 h after administration of the prodrug. By cross-breeding the BLG-NTR transgenic mice to a p53-deficient mouse strain, we have generated BLG-NTR transgenic mice on a p53 null background and tested NTR-mediated cell ablation in these mice. The transgenic mice lacking a functional p53 gene showed cell ablation at a similar level compared with p53 wild-type transgenic mice, showing that functional p53 is not required for CB1954-NTR mediated cell death. These results provide further support for using this system in anti-cancer therapy.  (+info)

TY - JOUR. T1 - Ethylcholine mustard aziridinium blocks the axoplasmic transport of acetylcholinesterase in cholinergic nerve fibres of the rat. AU - Kása, P.. AU - Hanin, I.. PY - 1985/7. Y1 - 1985/7. N2 - A cholinotoxin, ethylcholine mustard aziridinium ion, (AF64A) specifically and ireversibly blocks the intraaxonal transport of acetylcholinesterase in the rat. Impairment of the transport of this enzyme in the septo-hippocampal cholinergic fibres and in the sciatic nerve has been studied, using different doses of AF64A. It is demonstrated that the effect on the axonal transport is dose-dependent, but is not related to the mode of drug application. AF64A thus may exert its neurotoxic effects on cholinergic neurons at several target sites of action. In addition to the localized presynaptic mechanisms, it may also be compromising cholinergic function by inhibiting axonal transport in vivo.. AB - A cholinotoxin, ethylcholine mustard aziridinium ion, (AF64A) specifically and ireversibly blocks ...
article{1234402, author = {Dhooghe, Matthias and Kenis, Sara and Vervisch, Karel and Lategan, Carmen and Smith, Peter and Chibale, Kelly and De Kimpe, Norbert}, issn = {0223-5234}, journal = {EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY}, keyword = {Aziridinium salts,Aziridines,Ring opening,Triaminopropanes,Antimalarial agents,INTERMEDIATE AZIRIDINIUM SALTS,PLASMODIUM-FALCIPARUM,PURINE DERIVATIVES,CHIRAL AZIRIDINES,1-ALKYL-2-(BROMOMETHYL)AZIRIDINES,CHEMOTHERAPY,EPOXIDES,POTENT,ASSAY,IONS}, language = {eng}, number = {2}, pages = {579--587}, title = {Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores}, url = {http://dx.doi.org/10.1016/j.ejmech.2010.11.037}, volume = {46}, year = {2011 ...
Binary ethylenimine (BEI) is a preparation of aziridine. It can be produced by heating bromoethylamine hydrobromide or 2-aminoethyl hydrogen sulfate in the presence of sodium hydroxide (Gabriel method). It contains at least one three-membered ring which is very reactive because of the ring strain. It is used to inactivate the foot-and-mouth disease virus in vaccines for cattle, as well as other viruses and mycoplasma in blood samples. Contrary to early assumptions that ethylenimines only modified nucleic acids, it was found that trimeric ethyleimine also alters proteins in virus preparations, especially at higher pH values. The modification of the proteins affected viral particle uptake into cells. This should be taken into consideration when using BEI and other ethyleneimines as well. BEI is very hazardous since it attacks nucleic acids and proteins as described above. It can be neutralised by sodium thiosulfate; the thiosulfate is a nucleophile which opens the three-membered ring. The presence ...
S)-3-Amino-2-(1-hydroxy-2,2-dimethylprop-1-yl)-quinazolin-4(3H)-one (Q*NH2) was prepared from (L)-tert-leucine and its 3-acetoxyamino derivative (Q*NHOAc) used to aziridinate a range of alkenes. In the presence of titanium (IV) tert-butoxide, Q*NHOAc was found to convert styrene, indene, butadiene and tert-butyl acrylate with complete diastereoselectivity into the corresponding N-Q* substituted aziridines in good yield; aziridination of methyl acrylate and -methylstyrene was also highly diastereoselective. In the absence of titanium (IV) tert-butoxide, aziridination proceeded with poor diastereoselectivity in every case.;The quinazolinone (Q*) ring has proved to be invaluable in directing or assisting the course of ring-opening of the N-(Q*) aziridines produced above. Thus Q* as a substituent on nitrogen was found to be sufficiently electron-withdrawing to activate the aziridine ring towards attack by nucleophiles in the absence of acid. The C-4 carbonyl oxygen of the quinazolinone (Q*) was ...
article{1943629, abstract = {The difference in reactivity between the activated 2-bromomethyl-1-tosylaziridine and the nonactivated 1-benzyl-2-(bromomethyl)aziridine with respect to sodium methoxide was analyzed by means of DFT calculations within the supermolecule approach, taking into account explicit solvent molecules. In addition, the reactivity of epibromohydrin with regard to sodium methoxide was assessed as well. The barriers for direct displacement of bromide by methoxide in methanol are comparable for all three heterocyclic species under study. However, ring opening was found to be only feasible for the epoxide and the activated aziridine, and not for the nonactivated aziridine. According to these computational analyses, the synthesis of chiral 2-substituted 1-tosylaziridines can take place with inversion (through ring opening/ring closure) or retention (through direct bromide displacement) of configuration upon treatment of the corresponding 2-(bromomethyl)aziridines with 1 equiv of a ...
Several highly selective biochemical markers were used to assess the persistent central cholinergic dysfunction which accompanies administration of the cholinergic neurotoxin ethylcholine mustard aziridinium ion (AF64A). Rats received a single bilateral intracerebroventricular injection of AF64A (3 nmol/3 microliter/side) or vehicle and measurements were carried out in the cerebral cortices, hippocampi and corpora striata at 7 and 21 days postinjection. The drug binding sites of muscarinic cholinergic receptors, as revealed by high-affinity binding of (-)-[3H]quinuclidinyl benzilate (a classical muscarinic antagonist), [3H]pirenzepine (a selective antagonist of the putative M1 muscarinic receptor subclass) and (+)-[3H]cis-methyldioxolane (a potent muscarinic agonist), were not significantly affected by AF64A treatment. As reported previously, activity of the cholinergic synthetic enzyme choline acetyltransferase was reduced markedly (60-65%) in the hippocampi of AF64A-treated rats. A similar ...
The reaction of 2-naphthols with aziridines in the presence of AgOTf resulting in a dehydrative, formal [3+2] annulation is reported. The reaction allows the synthesis of functionalized benzoindolines, and tolerates a broad range of functional groups. A preliminary study on the mechanism of this reaction ind
Comprehensive supplier list for Aziridine, 1-(1,1-dimethylethoxy)-2,2,3-trimethyl-,Aziridine, 1-(1,1-dimethylethyl)-2,3-diphenyl-, cis-
TY - CHAP. T1 - Tissue distribution and intracerebral tumor penetration of 2,5-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZO, NSC 182986) in man. AU - Savaraj, Niramol. AU - Lu, K.. AU - Stewart, D.. PY - 1981/1/1. Y1 - 1981/1/1. UR - http://www.scopus.com/inward/record.url?scp=17544399898&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=17544399898&partnerID=8YFLogxK. M3 - Chapter. AN - SCOPUS:17544399898. VL - Vol. 22. BT - Proceedings of the American Association for Cancer Research. ER - ...
Limited examples of the successful ring expansion of aziridines with sulfonium ylides to generate azetidines are known, but typically result in functional groups on azetidine that are not broadly useful for downstream chemistry. Described here is an investigation into the scope of this reaction including the discovery that N-activated 2-methoxy ester functionalised aziridines are not compatible with this protocol. Advances have also been made in understanding the reactivity of azirines with rhodium carbenoids to generate azetines from successful ring expansion, or N-vinylimine from ring opening.. An alternative route to azetidines from the 1,3-cleavage of azabicyclo[1.1.0]butanes is described, along with a proposed route to highly functionalised azetidines with control over the absolute configuration at each step. Early success reacting a range of reagents with an azabicyclo[1.1.0]butane of moderate steric bulk has been shown, as well as early steps towards a novel azetidine 3-sulfonamide ...
The reaction of N-tosyl imines with in situ generated iodomethyllithium, with a simple and rapid experimental protocol, allows an efficient and general synthesis of aziridines. A reaction of a chiral aldimine derived from phenylalaninal proceeded with high diastereoselectivity. A mechanism to explain this novel reaction is proposed ...
Takase, S; Watanabe, M; Shiratori, O; and Hata, Y, An antagonistic effect between aziridine and diaziridine on their cytotoxic activities against l-1210 mouse leukemia cells. (1982). Subject Strain Bibliography 1982. 3043 ...
Reduction of (RS)-N-tert-butanesulfinyl α-halo imines with NaBH4 in THF, in the presence of 10 equiv of MeOH, and subsequent cyclization with KOH afforded the corresponding (RS,S)-N-(tert-butylsulfinyl)aziridines in quantitative yields. On the contrary, its epimer, (RS,R)-N-(tert-butylsulfinyl)aziridine was synthesized in good yields and diastereoselectivity by switchover of the reducing agent from NaBH4 to LiBHEt3 ...
The rich surface chemistry of mesoporous metal oxides is an important reason why they are widely used in applications such as catalysis, biomolecular separation, etc. At times the surface is modified or functionalized with organic species for stability or for a particular application. In this work, nanocast metal oxides (TiO2, ZrO2 and SnO2) and SiO2 were modified with amino-containing molecules using four different approaches, namely (a) covalent bonding of 3-aminopropyltriethoxysilane (APTES), (b) adsorption of 2-aminoethyl dihydrogen phosphate (AEDP), (c) surface polymerization of aziridine and (d) adsorption of poly(ethylenimine) (PEI) through electrostatic interactions. Afterwards, the hydrolytic stability of each functionalization was investigated at pH 2 and 10 by zeta potential measurements. The modifications were successful except for the AEDP approach which was unable to produce efficient amino-modification on any of the metal oxides used. The APTES, aziridine and PEI ...
Bakkali-Hassani, C.; Rieger, E.; Vignolle, J.; Wurm, F. R.; Carlotti, S.; Taton, D.: Expanding the scope of N-heterocyclic carbene-organocatalyzed ring-opening polymerization of N-tosyl aziridines using functional and non-activated amine initiators. European Polymer Journal 95, S. 746 - 755 (2017 ...
This thesis is focused on the development of new pincer complex-catalyzed transformations. Optimization of the catalytic properties (fine-tuning) was directed to increase the catalytic activity as well as the chemo-, stereo- and enantioselectivity of the complexes. This was achieved by varying the heteroatoms in the terdentate pincer ligand, by changing the electronic properties of the coordinated aryl moiety and by implementing chiral functionalities in the pincer complexes.. In the cross-coupling reaction of vinyl epoxides and aziridines with organoboronic acids the chemoselectivity of the reaction could be increased by employment of pincer complexes instead of commonly used Pd(0) catalysts. Furthermore, the introduction of a methoxy substituent in the aromatic subunit of the complex considerably increased the activity of the pincer complex catalyst.. Fine-tuning of the enantioselectivity in electrophilic allylation reactions was achieved by using a wide variety of new BINOL- and ...
报告题目:New Methods and Reagents for the Transition Metal-Free Direct Synthesis of Unprotected Aromatic Amines, Hydroxyarenes, Fused N-Heterocycles and Aziridines报告人:Dr. LászlóKürti报告时间:2020年1月6日(星期一)上午10:30-11:30报告地点:独墅湖校区912-1114会议室报告人简介:2015.06至今美国莱斯大学,终身副教授2010-2015美国德克萨斯大学西南医学中心,助理教授2006-2010美国哈佛大学,博士后2001-2006美国宾夕法尼亚大学,有机化学博士The Kürti labhas been exploring several fundamentally new strategies and methods for the creation of novel C-C and C-heteroatom (C-O, C-N and C-S) bonds that expand the t
Еремеев А.В.; Солодин И.В.; Лиепиньш Э.Э.; Костяновский Р.Г. Исследование методов синтеза азиридинов и азиринов на основе этил-beta,beta-бис(трифторметил)акрилата = Investigation of methods for the synthesis of aziridines and azirines on the basis of ethyl-beta,beta-bis(trifluoromethyl) acrilate. Химия гетероцикл.соед. 1984(7), 917-921; Chem.Heterocycl. Comp. (Engl. Ed.). 1984, 20(7), 744-748 ...
Bull Group , United Kingdom - The first preparation of iodoaziridines. The addition of diiodomethyllithium to N-Boc-imines affords these novel aziridines in high yields. The reaction proceeds in one-pot via a highly diastereoselective cyclisation of an a.
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
3-(Aziridin-1-ylmethyl)-1H-indole | C11H12N2 | CID 265359 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Two new bioreductive compounds, 9-[3-(2-nitro-1-imidazolyl)propylamino]acridine hydrochloride (NLA-1) and 9-[2-(2-nitro-1-imidazolyl)ethylamino]acridine hydrochloride (NLA-2), which behave as hypoxic cytotoxins and radiosensitizers, have been investi
This page contains information on the chemical Urea, 1-(2-(bis(1-aziridinyl)phosphinyl)vinyl)-3-phenyl- including: 5 synonyms/identifiers.
Trapencieris P.; Kalviņš I.; Kupče Ē.; Lukevics E. Synthesis of a New Aziridine Bicyclic System: 6,6-Diphenyl-5,7-dioxa-6-sila-1-azabicyclo[7.1.0]decane. J. Chem. Res. Part S 1996(3), 142-143 ...
Being focused on the research, development, production, trade and service of fine chemicals, Holdenchem now is a specialized manufacturer and trader of Imidazole series and aziridine series of products.
Being focused on the research, development, production, trade and service of fine chemicals, Holdenchem now is a specialized manufacturer and trader of Imidazole series and aziridine series of products.
TY - JOUR. T1 - Aziridinylbenzoquinone (AZQ) in the treatment of recurrent pediatric brain and other malignant solid tumors - A Pediatric Oncology Group phase II study. AU - Castleberry, R. P.. AU - Ragab, A. H.. AU - Steuber, C. P.. AU - Kamen, B.. AU - Toledano, S.. AU - Starling, K.. AU - Norris, D.. AU - Burger, P.. AU - Krischer, J. P.. PY - 1990/11. Y1 - 1990/11. N2 - To assess the response rates and toxicity of AZQ in children with recurrent brain and other malignant solid tumors, a phase II study was implemented by the Pediatric Oncology Group. Eligible patients received AZQ 18 mg/M2/week i.v. for 4 doses followed by a 2 week rest period. Each dose was given over four hours (1/3 over the initial 20 minutes). After the first year, the dosage was reduced to 13 mg/M2 due to myelotoxicity resulting in treatment delays. No objective responses were observed in 73 evaluable children with various noncentral nervous system tumors. Of the 91 patients with brain tumors, there were 4 CRs and 2 PRs ...
TY - JOUR. T1 - Reducible poly(amido ethylenimine)s designed for triggered intracellular gene delivery. AU - Christensen, Lane V.. AU - Christensen, L.. AU - Chang, Chien-Wen. AU - Kim, Won Jong. AU - Kim, Sung Wan. AU - Zhong, Zhiyuan. AU - Lin, C.. AU - Engbersen, Johannes F.J.. AU - Feijen, Jan. PY - 2006. Y1 - 2006. N2 - Poly(amido ethylenimine) polymers, a new type of peptidomimetic polymer, containing multiple disulfide bonds (SS-PAEIs) designed to degrade after delivery of plasmid DNA (pDNA) into the cell were synthesized and investigated as new carriers for triggered intracellular gene delivery. More specifically, three SS-PAEIs were synthesized from Michael addition reactions between cystamine bisacrylamide (CBA) and three different ethylene amine monomers, i.e., ethylenediamine (EDA), diethylenetriamine (DETA), or triethylenetetramine (TETA). Complete addition reactions were confirmed by 1H NMR. The molecular weight, buffer capacity, and relative degree of branching for each SS-PAEI ...
TY - JOUR. T1 - Mechanism of enhanced sensitivity of linear poly(ethylenimine)-carbon black composite detectors to carboxylic acid vapors. AU - Tillman, Eric S.. AU - Lewis, Nathan S.. PY - 2003/11/15. Y1 - 2003/11/15. N2 - Enhanced sensitivity towards volatile carboxylic acid vapors is obtained when the basic, amine-containing polymer, linear poly(ethylenimine), l-PEI, is used as the insulating component in a carbon black-polymer composite vapor detector. Specifically, at a partial pressure of analyte corresponding to 1% of its vapor pressure at room temperature, the signal-to-noise ratio for detection of acetic acid is 103 times larger than that for non-acidic organic vapors. Measurements of the mass uptake, thickness change, and electrical conductivity of such composites have been performed to elucidate the mechanism of this sensitivity enhancement towards volatile carboxylic acid vapors. These data have allowed quantification of the relative contributions of electrical percolation effects, ...
Ovarian cancer remains the most lethal gynaecological cancer mainly due to the lack of reliable biomarkers and eventual development of chemo-resistance. This emphasizes the need for better therapies. Ovarian cancer is considered as an immunogenic tumour and adoptive immunotherapy is a promising treatment strategy. However, co-inhibitory molecules such as programmed death-ligand 1 (PD-L1), highly expressed on ovarian cancer cells interacts with its receptor, programmed death-1 (PD-1), expressed on T cells, causing immunosuppression. The aim of this Ph.D. was to 1) develop more efficient and targeted gene delivery agents by functionalizing poly(ethylenimine) (PEI) with various hydrophobic groups and folic acid (FA) targeting ligand, 2) deliver PD-L1 small interfering RNA (siRNA) or short hairpin RNA (shRNA) into ovarian cancer cells to block PD-1/PD-L1 interactions and 3) to study how T cell function and anti-tumour activity are affected as a consequence of PD-L1 knockdown. 4) In addition, ...
68307-89-1 - Aziridine, homopolymer, reaction products with epichlorohydrin - Similar structures search, synonyms, formulas, resource links, and other chemical information.
BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition ...
Chiral N, N - and N,O-Bidentate Anionic Ligands. Preparation, Metal Complexation, and Evalution in the Asymmetric Aziridination of Olefins ...
Peptide isosteres are important tools for the understanding of peptide function and for the development of drugs. (E)-Alkene peptide isosteres are particularly useful due to their close geometric match of the amide bond structure. We developed a method for the generation of a small library of (E)-alkene peptide isosteres on solid support via cuprate mediated SN2? ring opening of allylic BUS-aziridines. We also studied the selectivity for the opening of these aziridines in the solution phase. Halenaquinone is a marine natural product that was first isolated in 1983 from the Pacific sponge Xestosongia exigua. We realized the synthesis of a thiophene-containing analog, thio-halenaquinone. The key steps include an alkynyl ketone-benzocylcobutane Diels-Alder reaction to construct the naphthalene subunit, a Heck cyclization to form the quaternary carbon, and a ring closing metathesis to install the final ring. This compound showed an IC90 ~5 µM against Pfnek-1 and an analog that had an IC90 ~3 µM. ...
Synthesis provides the opportunity to design and prepare specific molecules whilst exploring novel processes that further develop the field of organic chemistry. In this context, our programme has concentrated on new and selective carbon-carbon bond forming strategies for the preparation of functionalised synthetic Intermediates. A summary of projects currently under investigation is outlined below:. Alkynylboronate Cycloadditions. Aromatic boronic acids and esters are extremely useful and versatile substrates in modern organic chemistry. We have developed a strategically novel approach to these compounds through cycloaddition reactions of alkynylboronates. To date, this approach has allowed us to generate boronic esters that are connected to benzene, quinone, pyridine, pyrazole, isoxazole and pyridazine scaffolds.. [3 + 3] Annelation Reactions. We have designed an efficient method for the synthesis of piperidines and pyrans by the addition of conjunctive reagents to aziridines and epoxides. ...
1ICR: The structure of Escherichia coli nitroreductase complexed with nicotinic acid: three crystal forms at 1.7 A, 1.8 A and 2.4 A resolution.
Individuals with deficiencies of these factors or platelets exhibit to bleed; they do not bleed more very likely than people without these conditions, but it is justifiable more difficult allowing for regarding the clot to form, and bleeding cannot be stopped easily. J Biol Chem 282:12377В-12387 Schurigt U, Schad C, Glowa C, Baum U, Thomale K, Schnitzer JK, Schultheis M, Schaschke N, Schirmeister T, Moll H (2010) Aziridine-2,3-dicarboxylate-based cysteine cathepsin inhibitors bring about apartment death in Leishmania crucial associated with accumulation of debris in autophagy- kindred lysosome-like vacuoles. What if benzol levels are really uttermost greater discount pilex 60 caps with mastercard prostate cancer oncologist. In physiological terms, interactions between natural networks result in changes chief to another form of equilibrium that okay better coping with the unfamiliar condition. Morbidity statistics are revised less frequently because of the formidableness in defining or obtaining ...
ACKNOWLEDGMENTS. The authors are thankful for the support of the Science and Technology National Council (CONACyT) by the SNI appointment received by the principal author and to the (PFCE) 2016 Educational Quality Strengthening Program.. REFERENCES CITED. Abou-Elela, S. I., Nasr, F. A., Ibrahim, H. S., Badr, N. M., and Askalany, A. R. M. (2008). Pollution prevention pays off in a board paper mill, Journal of Cleaner Production 16(3), 330-334. DOI: 10.1016/j.jclepro.2006.07.045. Ackermann, C., Gottsching, L., Pakarinen, H. (2000). Papermaking potential of recycled fiber, in: Recycled Fiber and Deinking, Göttsching, L., and Pakarinen, H. (eds.), Papermaking Science and Technology, Book 7; Fapet Oy: Jyväskylä, Finland, pp. 359-439.. Alince, B., and Van de Ven, T. G. M. (1993). Kinetics of colloidal particle deposition on pulp fibers 2. Deposition of clay on fibers in the presence of poly(ethylenimine), Colloids and Surfaces A: Physicochemical and Engineering Aspects 71(1), 105-114. DOI: ...
We sought to judge the partnership between cell department and proteins appearance when using business poly(ethylenimine) (PEI)-based polyplexes. But when the polyplex-exposed people was examined for the quantity of department in the protein-expressing subpopulation it had been observed that significant amounts of appearance had happened in the lack of department. Certainly in HeLa S3 cells […]. ...
1.Zhang, J.; Hoye, T. R. Divergent reactivity during the trapping of benzynes by glycidol analogs: ring cleavage via pinacol-like rearrangements vs oxirane fragmentations. Org. Lett. 2019, 21, 2615-2619. 2.Shen, H.; Xiao, X.; Hoye, T. R. Benzyne cascade reactions via benzoxetenonium ions and their rearrangements to o-quinone methides. Org. Lett. 2019, 21, 1672-1675. 3.Arora, S.; Palani, V.; Hoye, T. R. Reactions of diaziridines with benzynes give n-arylhydrazones. Org. Lett. 2018, 20, 8082-8085. 4.Wang, Y.; Zheng, L.; Hoye, T. R. Sulfonamide-trapping reactions of thermally generated benzynes. Org. Lett. 2018, 20, 7145-7148. 5.Xiao, X.; Wang, T.; Xu, F.; Hoye, T. R. Cu(I)-mediated bromoalkynylation and hydroalkynylation reactions of unsymmetrical benzynes: complementary modes of addition. Angew. Chem. Int. Ed. Engl. 2018, 57, 16564-16568. ...
A dental material which is curable in a first stage to an elastic phase in which the material can be worked mechanically or surpluses removed, and in a second stage to its final form, comprising: (a) at least one polyfunctional epimine (aziridine); (b) at least one ethylenically unsaturated monomer; (c) at least one catalyst for the hot, cold, or light polymerization of the ethylenically unsaturated monomer; and (d) at least one catalyst to accelerate the polymerization of epimine (a), but which does not however influence the polymerization of (b).
CP000386.PE141 Location/Qualifiers FT CDS complement(147289..148863) FT /codon_start=1 FT /transl_table=11 FT /locus_tag=Rxyl_0143 FT /product=SSS sodium solute transporter superfamily FT /note=TIGRFAM: SSS sodium solute transporter superfamily; FT PFAM: Na+/solute symporter; KEGG: gka:GK0928 sodium:solute FT symporter FT /db_xref=EnsemblGenomes-Gn:Rxyl_0143 FT /db_xref=EnsemblGenomes-Tr:ABG03122 FT /db_xref=GOA:Q1AZQ6 FT /db_xref=InterPro:IPR001734 FT /db_xref=InterPro:IPR038377 FT /db_xref=UniProtKB/TrEMBL:Q1AZQ6 FT /protein_id=ABG03122.1 FT /translation=MSDRAIATIFFVLIIVLTLGITAWAARRNKDTAHHYVAGGEIKGW FT QNGLAISGDYLSAASFLGIAGSIALTGFSGFYLSIGFLVAYLVVLLLVAEPLRNLGKYT FT FADMLAARFNLRSVRSAAALSTIAISTFYMIAQMVGAGALIELLLGLPYVASVVIIGVL FT MTIYIAAGGMVATTWIQIVKAVLLISGTLALSIAVLAQFGFNPVAIFDRVEAELGPEMV FT LPPPPEGFVSGIDVVSLNIALVFGTAGLPHILMRFLTVPDAKTARNSIIVATWIIGLFY FT LMTPIMGYGAALLVGQDVIAEQNPAGNTAAPQLAGELGGPIFLAFISAVAFATIVAVVA FT GLVIAASSAFAHDFYTNVIRGGEASEQEQFRAARIAAVAVSLGAMFLAIFARDFNVSFL FT ...
6EEA: Bioreductive 4-hydroxy-3-nitro-5-ureido-benzenesulfonamides selectively target the tumor-associated carbonic anhydrase isoforms IX and XII and show hypoxia-enhanced cytotoxicity against human cancer cell lines.
ZHU Li-Ping , YIN Yan , XING Jing , LI Chen , KOU Lei , HU Bi , WU Zhi-Wei , WANG Jian-Jun , XU Gen-Xing Cancer science 100(10), 1986-1990, 2009-10-10 医中誌Web 参考文献32件 被引用文献1件 ...
The ultimate value of the enzyme-directed bioreductive drug development concept in terms of individualizing patient therapy will depend upon the existence of a strong correlation between the activity of specific enzymes and antitumor responses in vivo. In view of the complex nature of MMC activation in conjunction with conflicting evidence of correlations between tumor response and DTD activity, it has been proposed that this concept be remodeled (29) . With regards to the enzyme DTD, controversy surrounds both its role in the activation of MMC and the correlation between antitumor responses in vitro and in vivo and DTD activity. In terms of predicting tumor response in vivo based upon DTD activities, only a limited number of studies have been published (26 , 27) , and of these, the number of xenografts evaluated has been too small to obtain statistically relevant information. This study has used a large panel of human tumor xenografts that have a broad spectrum of both DTD activity and ...
Fingerprint Dive into the research topics of The conjugation of diphtheria toxin T domain to poly(ethylenimine) based vectors for enhanced endosomal escape during gene transfection. Together they form a unique fingerprint. ...
TY - JOUR. T1 - Enantioselective Aziridination of Alkenes with N-Aminophthalimide in the Presence of Lead Tetraacetate-Mediated Chiral Ligand. AU - Yang, Kung Shou. AU - Chen, Kwunmin. PY - 2002/4/4. Y1 - 2002/4/4. N2 - matrix presented Reaction of various N-enoyl oxazolidinones 5a-f with N-aminophthalimide and lead tetraacetate in the presence of camphor-derived chiral ligands provides the desired N-phthalimidoaziridines 6a-f in good to high enantiomeric excess (67-95% ee) at 0°C within 15 min. The absolute stereochemistry of the corresponding aziridine derivatives was established by chemical correlations.. AB - matrix presented Reaction of various N-enoyl oxazolidinones 5a-f with N-aminophthalimide and lead tetraacetate in the presence of camphor-derived chiral ligands provides the desired N-phthalimidoaziridines 6a-f in good to high enantiomeric excess (67-95% ee) at 0°C within 15 min. The absolute stereochemistry of the corresponding aziridine derivatives was established by chemical ...
Bacterial nitroreductase enzymes that can efficiently catalyse the oxygen-independent reduction of prodrugs originally developed to target tumour hypoxia offer great potential for expanding the therapeutic range of these molecules to aerobic tumour regions, via the emerging cancer strategy of gene-directed enzyme prodrug therapy (GDEPT). Two promising hypoxia prodrugs for GDEPT are the dinitrobenzamide mustard PR-104A, and the nitrochloromethylbenzindoline prodrug nitro-CBI-DEI. We describe here use of a nitro-quenched fluorogenic probe to identify MsuE from Pseudomonas aeruginosa as a novel nitroreductase candidate for GDEPT. In SOS and bacteria-delivered enzyme prodrug cytotoxicity assays MsuE was less effective at activating CB1954 (a first-generation GDEPT prodrug) than the
Virus-directed enzyme prodrug therapy (VDEPT) utilising the bacterial enzyme nitroreductase delivered by a replication-defective adenovirus vector to activate the prodrug CB1954 is a promising strategy currently undergoing clinical trials in patients with a range of cancers. An understanding of the
NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, CB 1954 [5-(aziridin-1-yl)-2,4-dinitrobenzamide] and EO9 [5-(1-aziridinyl)-3-(hydroxymethyl)-2-(3-hydroxy-1-propenyl)-1- methyl-1H-indole-4,7-dione]. By using Escherichia coli-expressed quinone reductases and evaluating them under identical conditions, we confirmed previous finding showing that the human enzyme is not as effective as the rat enzyme in reducing CB 1954 and EO9, although the two enzymes have similar NAD(P)H-menadione reductase activities. Interestingly, although the amino acid sequence of mouse quinone reductase is more homologous to that of the rat enzyme, we found that the mouse enzyme behaves similarly to the human enzyme in its ability to reduce these compounds and ...
Methyl-substituted piperidines, oxanes, 1,3-dioxanes, and cyclohexanones were studied by photoelectron spectroscopy (pes) to determine the mechanism by which alkyl groups stabilize radical cations. Hyperconjugation was found to be the dominant mechanism, while inductive effects and charge-induced polarization were indicated to be less effective. N-Arylazacycloalkanes were studied by pes to correlate solution basicities with ionization potentials (IPs). Conformational analysis of these compounds indicated that aryl-substituted aziridines are coplanar (conjugating) in all cases studied, while ortho substituent(s) may cause rotation and loss of conjugation between the lone pair and the phenyl ring as the amine ring size is increased. N-Phenylpiperidine was indicated to be non-coplanar, despite the lack of ortho substituents. Pes studies of phencyclidine and a number of its analogs demonstrate that the amine lone pair IP changes predictably, depending on the nature and location of the substituent. The
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PubMed journal article Preparation of a poly(ethyleneimine) embedded phenyl stationary phase for mixed-mode liquid chromatograph were found in PRIME PubMed. Download Prime PubMed App to iPhone or iPad.
TY - JOUR UR - http://lib.ugent.be/catalog/pug01:2100766 ID - pug01:2100766 LA - eng TI - Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type additions across α-chloro-N-sulfinylimines PY - 2012 JO - (2012) ORGANIC & BIOMOLECULAR CHEMISTRY SN - 1477-0520 PB - 2012 AU - Callebaut, Gert 002004109623 802000651653 AU - Mangelinckx, Sven LA24 001996036896 AU - Kiss, Lorand AU - Sillanpaa, Reijo AU - Fulop, Ferenc AU - De Kimpe, Norbert AB - The efficient asymmetric synthesis of new chiral gamma-chloro-alpha,beta-diamino acid derivatives via highly diastereoselective Mannich-type reactions of N-(diphenylmethylene) glycine esters across a chiral alpha-chloro-N-p-toluenesulfinylimine was developed. The influence of the base, LDA or LiHMDS, used for the formation of the glycine enolates, was of great importance for the anti-/syn-diastereoselectivity of the Mannich-type reaction. The gamma-chloro-alpha,beta-diamino acid ...
786-06-1 - ZJNSELYCQTWFOO-UHFFFAOYSA-N - Phosphinic amide, P,P-bis(1-aziridinyl)-N-(6-methoxy-2-methyl-4-pyrimidinyl)- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Solid tumors provide an environment conducive to bioreduction due to hypoxia and overexpression of bioreductive enzymes. Therefore, TDDS were designed with various substituents to modulate bioreductive activation. TDDS contain a quinone-based carrier coupled to the model drug, melphalan methyl ester (MME). Controlled bioreductive activation of TDDS can lead to specific drug release only at the tumor sites and hence reduce toxicity during systemic distribution. The rate and extent of bioreductive activation of TDDS was determined in presence of DT-diaphorase, xanthine oxidase, human breast tumor cells (MCF-7) and colon tumor cells (Caco-2). Stability of TDDS under aqueous buffer conditions and in the presence of glutathione was also evaluated. Anticancer activity of TDDS was determined based on alkylating activity, cytotoxicity and apoptotic induction in both the tumor cell lines. Results show that all TDDS especially CH3-TDDS improved stability of melphalan under pH 7.4. H-TDDS possessed ...
Microsoft Azure Administrator Verified Practice Cram & AZ-104 Study Pdf Dumps & Microsoft Azure Administrator Exam Training Dumps, Also our soft test engine and app test engine can have extra functions which AZ-104 exam questions answers not only provide you valid questions answers but also simulate the real test scene and set timed practicing, Our three versions of Microsoft AZ-104 valid questions can make all buyers satisfying, As the most correct content, our AZ-104 New Test Test pdf practice is also full of appealing benefits.
The report describes the nitrosochlorination of fluorinated olefins in methanol at -70C; the reaction of CF2=CF2 and NOCl; propylene and UO2(NO2)2:H2O:N2O4; the synthesis of CF3CF2CF2CHOHCH2NH2, perfluoropropyl ethylenimine; the reaction of NO and CF2Cl-CFClI, CF2=CFCl, CF2=CCl2, CFCl=CFCl, and perfluorocyclobutene.(*HALOGENATED HYDROCARBONS
The non download the making of psychological, only, which remains parallels still possible to each separate, eating a such and more perceivable action, has the opinions of Platone, and assumes the non relation of their aptitude. 2019; d reservoirs; they reply profit, as a philosophical sea to exist their sancti, and introduce the inflexible, or be useless agencies, by a more several mind of stimet. insensibly not, fully, our moral darknesses abstract punished with our many, that the sufficient know considered only for the game of the end; and that the supercritical function of pleasure has to be Diaziridines to contend the rises of dog.
As we all know there are two types of prominent β-lactamases in pathogenic bacteria the serine and the metallo enzymes which have a zinc atom in the active site. The appearance of metallo-β-lactamases (MBLs) have increased in frequency and concern over the past years and can inactivate essentially all penicillins, cephalosporins, and carbapenems, thereby threatening the majority of clinically used antibiotics. Especially the emergence and widespread global distribution of Gram- negative pathogens harboring the NDM-1 MBL is really a concern. There is a growing need for inhibitors of MBLs that can be given as co-drugs.. Their approach towards AMA allowed the determination of the absolute conformation and provides access to analogues. It uses some nice aziridine building blocks derived from D or L-serine.. ...
R. Talaty, A . R. Clague, M. 0. Agho, M. N. Deshpande, P. M. Courtney, D. H. Burger. and E. F. Roberts, J. Chem. ,Chem. , 1980,889. W. D. Rudorf, Tetrahedron, 1980,36, 1791. 200This forms the last step in a mild, general method for preparation of oxazolines, starting from the conversion of a wide range of carboxylic acids into their acyl-imidazoles, with subsequent addition of aziridine, to give quantitative yields of the corresponding N-acyl-aziridines (260). 201The cell consisted of a platinum anode and a graphite cathode, using Bun4 C104 in MeOH, CH2C12,or MeCN as the electrolyte; yields of up to 80% have been reported, with low consumption of electricity. A. Donnelly and D. E. Maloney, Tetrahedron, 1979,35, 2875. 6o 61 J. A. Donnelly and D. E. Maloney, Tetrahedron, 1979, 35, 2883. S. Akabori, M. Ohtomi, and S. Yatabe, Bull. Chem. SOC. , 1980, 53, 1463. 9 J (47) (48) Scheme 6 (49) Two groups, working independently, have simultaneously published descriptions of epoxyannulation procedures, ...
R. Talaty, A . R. Clague, M. 0. Agho, M. N. Deshpande, P. M. Courtney, D. H. Burger. and E. F. Roberts, J. Chem. ,Chem. , 1980,889. W. D. Rudorf, Tetrahedron, 1980,36, 1791. 200This forms the last step in a mild, general method for preparation of oxazolines, starting from the conversion of a wide range of carboxylic acids into their acyl-imidazoles, with subsequent addition of aziridine, to give quantitative yields of the corresponding N-acyl-aziridines (260). 201The cell consisted of a platinum anode and a graphite cathode, using Bun4 C104 in MeOH, CH2C12,or MeCN as the electrolyte; yields of up to 80% have been reported, with low consumption of electricity. A. Donnelly and D. E. Maloney, Tetrahedron, 1979,35, 2875. 6o 61 J. A. Donnelly and D. E. Maloney, Tetrahedron, 1979, 35, 2883. S. Akabori, M. Ohtomi, and S. Yatabe, Bull. Chem. SOC. , 1980, 53, 1463. 9 J (47) (48) Scheme 6 (49) Two groups, working independently, have simultaneously published descriptions of epoxyannulation procedures, ...
When it is synthesized for commercial use, taurine is made from isetheonic acid or through the reaction of aziridine with sulfurous acid. Taurine occurs naturally in the human body, and it is found...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
CP001022.PE191 Location/Qualifiers FT CDS_pept complement(209651..210208) FT /codon_start=1 FT /transl_table=11 FT /locus_tag=Exig_0193 FT /product=nitroreductase FT /note=PFAM: nitroreductase; KEGG: bsu:BSU08480 FT hypothetical protein FT /db_xref=EnsemblGenomes-Gn:Exig_0193 FT /db_xref=EnsemblGenomes-Tr:ACB59679 FT /db_xref=GOA:B1YHE7 FT /db_xref=InterPro:IPR000415 FT /db_xref=InterPro:IPR026021 FT /db_xref=InterPro:IPR029479 FT /db_xref=UniProtKB/TrEMBL:B1YHE7 FT /protein_id=ACB59679.1 FT /translation=MNTRQLILERRSVRAYTDQPVPNEMIEEILEAAIYAPTHKLREPW FT RFVLVNEESQERYVDQLMTLLAKRGQLDQKTDEQRQMMRQKFADVPVYLTVLYEVKGTE FT DQQMEDLLATAAMIQNVQLLATELGLGCCWKSGKHWFTEEYAEMIGASENERVAGIIQF FT GWPALIPPLKKRTAARDKLTHF atgaacaccc gacaactgat tttagaacga cgatccgtcc gtgcttacac cgatcagccg 60 gttccaaatg aaatgattga agaaattctc gaagccgcca tctatgctcc gactcataaa 120 ttgcgtgaac cttggcgatt tgtcctcgtt aacgaagaaa gccaagagcg gtatgtcgac 180 caattgatga cgctgcttgc caagcgggga cagctggatc aaaaaacaga cgaacaacgc 240 ...
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It is used industrially for the synthesis of aziridine itself. The original Wenker synthesis of aziridine itself takes place in ... The Wenker synthesis is an organic reaction converting a beta amino alcohol to an aziridine with the help of sulfuric acid. ... This salt is then reacted with sodium hydroxide in the second step forming aziridine. The base abstracts an amine proton ... Steuerle, Ulrich; Feuerhake, Robert (2006). "Aziridines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. ...
Branched PEI can be synthesized by the ring opening polymerization of aziridine. Depending on the reaction conditions different ... Steuerle, Ulrich; Feuerhake, Robert (2006). "Aziridines". Ullmann's Encyclopedia of Industrial Chemistry. Weinheim: Wiley-VCH. ...
2007). Aziridines and Epoxides in Organic Synthesis. p. 120. ISBN 978-3-527-31213-9. The quinazoline is prepared from the ... With alkenes, nitrenes react to form aziridines, very often with nitrenoid precursors such as nosyl- or tosyl-substituted [N-( ... Watson, Iain D. G.; Yu, Lily; Yudi, Andrei K. (2006). "Advances in Nitrogen Transfer Reactions Involving Aziridines". Acc. Chem ... result in the same trans-aziridine product, suggesting a two-step reaction mechanism. The energy difference between triplet and ...
Aziridines include thiotepa, mytomycin and diaziquone (AZQ). Cisplatin and derivatives include cisplatin, carboplatin and ... The subtypes of alkylating agents are the nitrogen mustards, nitrosoureas, tetrazines, aziridines, cisplatins and derivatives, ...
Aziridine-2,3-dione has an infrared absorption band at 1954 cm−1. The term "oximide" has also been used for oximes. Derivatives ... Its core is a three member heterocycle, aziridine. In 1886 Ost and Mente claimed to produce oximide by the reaction of oxamic ... Derivatives made this way are methyl, isopropyl and phenylethyl-aziridine-2,3-dione. These compounds are unstable at higher ... Aoyama, Hiromu; Sakamoto, Masami; Omote, Yoshimori (September 1980). "Aziridine-2,3-diones". Journal of the American Chemical ...
Note that with aziridines, ring opening can result in a different 1,3-dipole, in which a C-N bond (rather than the C-C bond) ... Cardoso, Ana L.; Pinho e Melo, Teresa M. V. D. (2012). "Aziridines in Formal [3+2]Cycloadditions: Synthesis of Five-Membered ... This is generally done by ring opening of an aziridine, and subsequent trapping by a dipolarophile before the stereochemistry ... Azomethine ylides can be generated from ring opening of aziridines. In accordance with the Woodward-Hoffmann rules, the thermal ...
... amino alcohols to the corresponding aziridines with diethoxytriphenylphosphorane". The Journal of Organic Chemistry. 51 (1): 95 ...
... ketononestrol aziridine) and antiestrogen (tamoxifen aziridine) in the human estrogen receptor". The Journal of Biological ... "Tamoxifen aziridines: effective inactivators of the estrogen receptor". Endocrinology. 109 (4): 1298-1300. doi:10.1210/endo-109 ...
"Recent Advances in the Stereoselective Synthesis of Aziridines". Chemical Reviews. 114 (16): 7881-7929. doi:10.1021/cr400553c. ...
Chemotherapy Aziridine v t e. ...
"Directed Nickel-Catalyzed Negishi Cross Coupling of Alkyl Aziridines". Journal of the American Chemical Society. 135 (36): ...
Aziridine occurs by the cyclization of chloroethylamine; piperazines are formed by cyclization of a two-ethylene unit compound ...
Cyclopropenes, aziridines and cyclobutanes may be formed in a similar manner. Carbon acids which can be deprotonated by sodium ...
It can also cyclize 2-aminoalcohols to aziridines and to convert α,β-unsaturated carboxylic acids to α,β-unsaturated bromides. ... doi:10.1002/047084289X.rd448.pub2 H. Suzuki; H. Tani (1984). "A mild cyclization of 2-aminoalcohols to aziridines using ...
... and Aziridine Biosynthesis". Chem. Rev. 112 (3): 1681-1709. doi:10.1021/cr200073d. PMC 3288687. PMID 22017381. Boron WF (2003 ...
... (BEI) is a preparation of aziridine. It can be produced by heating bromoethylamine hydrobromide or 2- ...
It is made from aziridine and mesoporous silica. "Can we make tailpipes that capture CO2?". HowStuffWorks. 2008-05-27. ...
Diastereopure azomethine ylides are generated by electrocyclic ring opening of aziridines, and then rapidly trapped with strong ... Huisgen, Rolf; Scheer, Wolfgang; Huber, Helmut (1967). "Stereospecific Conversion of cis-trans Isomeric Aziridines to Open- ...
It is manufactured by heating aziridine with thiophosphoryl chloride.[citation needed] Thiotepa is indicated for use in ...
Alternatively aziridine intermediate 9 directly forms the end=product. The formation of the nitrene intermediate 10 is ruled ...
9) The aza-Payne rearrangement may be effected in either the "forward" (epoxide to aziridine) or "reverse" (aziridine to ... Electron-poor aziridines undergo the reverse rearrangement in the presence of hydride base, while the corresponding epoxy ... Aza- and thia-Payne rearrangements of aziridines and thiiraniums, respectively, are also known. Under basic, protic conditions ...
TACN is one of the oligomers derived from aziridine, C2H4NH. Other members of the series include piperazine, C4H8(NH)2, and the ...
It is the sulfur analogue of an epoxide or aziridine. They are also known as thiiranes, olefin sulfides, thioalkylene oxides, ...
Intramolecular reactions of haloamines X-(CH2)n-NH2 give cyclic aziridines, azetidines and pyrrolidines. N-alkylation is a ...
Alternatively, they can be obtained by oxidation of the corresponding aziridine. Photolysis of azirines (under 300 nm) is a ... compounds containing a nitrogen atom and related to the saturated analogue aziridine. They are highly reactive yet have been ...
A direct approach involves the reaction of aziridine with sulfurous acid. In 1993, about 5,000-6,000 tons of taurine were ...
... aziridine 2-carboxylates, and aziridine 2-phosphonates. Many of these same transformations can be carried out with tert- ... aziridine-2-carboxylic Acids". Journal of Organic Chemistry. 59 (12): 3243-3245. doi:10.1021/jo00091a001. Davis, Franklin A.; ... aziridine 2-Carboxylate Esters from Sulfinimines (N-Sulfinyl Imines)". Journal of Organic Chemistry. 64 (20): 7559-7567. doi: ... "Asymmetric Synthesis of Aziridine 2-Phosphonates from Enantiopure Sulfinimines (N-Sulfinyl Imines). Synthesis of α-Amino ...
The reaction also provides substituted aziridines from simple aldehydes and ketones with high yield and diastereoselectivity. 1 ...
Monomers with a three-member ring structure - such as epoxides, aziridines, and episulfides - undergo anionic ROP. A typical ...
Nitrogen mustards react via an initial cyclization to the corresponding quaternary aziridine salt. The rate of this reaction is ...
Aziridines are organic compounds containing the aziridine functional group, a three-membered heterocycle with one amine (-NR-) ... Alkene + DPH → R h 2 ( C O 2 R ) 4 {\displaystyle {\xrightarrow {Rh_{2}(CO_{2}R)_{4}}}} Aziridine For instance, Ph-Aziridine-Me ... The De Kimpe aziridine synthesis allows for the generation of aziridines by reacting an α-chloroimine with a nucleophile, such ... which affords aziridines. Aziridines are obtained by treating a mono-, di-, tri- or tetra- substituted alkene (olefin) with O-( ...
Aziridine containing compounds also appear to be similarly dangerous. Binary ethylenimine, a dimeric form of aziridine " ... Its derivatives, also referred to as aziridines, are of broader interest in medicinal chemistry. The bond angles in aziridine ... Aziridine is highly toxic with an LD50 of 14 mg (oral, rats). It is a skin irritant. As an alkylating agent, it is also a ... Aziridine is less basic than acyclic aliphatic amines, with a pKa of 7.9 for the conjugate acid, due to increased s character ...
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Adducts derived from P(NMe2)3 and α-ketoesters are effectively intercepted by N-sulfonyl imines, affording a range of aziridine ... A mild, convenient protocol for the synthesis of cis-aziridines employs a catalytic amount of Br nsted acid. Diazo compound ... The tertiary amine DABCO catalyzes the reaction of imines with phenacyl bromide derivatives to afford functionalized aziridines ... PF6 to produce the corresponding aryl aziridine carboxylates in high yields with excellent cis-diastereoselectivity.. J. S. ...
... Satoshi Minakata, Yuriko Okada, Yoji Oderaotoshi ...
The reaction of 2-naphthols with aziridines in the presence of AgOTf resulting in a dehydrative, formal [3+2] annulation is ... A preliminary study on the mechanism of this reaction indicates an SN1-type ring-opening of aziridines. This method is ... AgOTf-catalyzed dehydrative [3+2] annulation of aziridines with 2-naphthols T. Kaicharla, A. Jacob, R. G. Gonnade and A. T. ... The reaction of 2-naphthols with aziridines in the presence of AgOTf resulting in a dehydrative, formal [3+2] annulation is ...
Two alternative and complementary one-pot procedures for the direct transformation of 2-amino alcohols to N-tosyl aziridines ... Short and Efficient Synthesis of Optically Active N-Tosyl Aziridines from 2-Amino Alcohols. Lothar W. Bieber * and Maria C. F. ... Bieber, L.W.; De Araújo, M.C.F. Short and Efficient Synthesis of Optically Active N-Tosyl Aziridines from 2-Amino Alcohols. ... Two alternative and complementary one-pot procedures for the direct transformation of 2-amino alcohols to N-tosyl aziridines ...
A novel and selective fluoride opening of aziridines by XtalFluor-E. synthesis of fluorinated diamino acid derivatives.. [ ... The method based on the selective aziridine opening by fluoride has been generalized to afford access to mono- or bicyclic ... or cyclohexane carboxylate has been developed through a novel and efficient fluoride opening of an activated aziridine ring ... proceeded through a stereoselective aziridination of the olefinic bond of a bicyclic lactam and regioselective aziridine ring ...
Cyclophellitol epoxides and aziridines are recently established covalent glycosidase inactivators. Inspired by the application ... in complex with beta Cyclophellitol Aziridine probe KY358. *DOI: 10.2210/pdb5NPE/pdb ...
Ficellomycin is an aziridine antibiotic produced by Streptomyces ficellus, which displays high in vitro activity against Gram- ... Ficellomycin is an aziridine antibiotic produced by Streptomyces ficellus, which displays high in vitro activity against Gram- ... Ittah Y, Sasson Y, Shahak I, Tsaroom S, Blum J (1978) A new Aziridine synthesis from 2-azido alcohols and tertiary phosphines. ... Ismail F, Levitsky D, Dembitsky V (2009) Aziridine alkaloids as potential therapeutic agents. Eur J Med Chem 44(9):3373-3387 ...
... aziridine-2-carboxylic acid , C7H9NO4-2 , CID 3460800 - structure, chemical names, physical and chemical properties, ...
The C-4 carbonyl oxygen of the quinazolinone (Q*) was found to participate in the aziridine ring-opening under some conditions ... Finally, the sense of regioselectivity in the ring-opening of the methyl acrylate-derived aziridine can be changed by forming a ... Thus Q* as a substituent on nitrogen was found to be sufficiently electron-withdrawing to activate the aziridine ring towards ... The two N-invertomers of the indene-derived aziridine were separately ring-opened by hydrogen chloride with very different ...
160-5000 and a cationic polymerization retarding agent(s). A two-component cationically-curable aziridine polyether-based ... and an aziridine salt(s) of an acid, and a base component including a mixture of N-alkylaziridine polyol ethers with imino ... composition comprises: (1) a catalyst component comprising: (a) 0.01-50 wt.% acid(s); (b) 0.01-99.5 wt.% aziridine salt(s) of ... A two-component cationically-curable aziridine polyether-based composition comprises a catalyst component, including an acid(s ...
... ... Occupational asthma and contact dermatitis in a spray painter after introduction of an aziridine cross-linker. Environmental ... dermatitis and respiratory difficulty characterized by small airways obstruction shortly after the polyfunctional aziridine ...
Mechanistic Approaches to Asymmetric Synthesis of Aziridines from Guanidinium Ylides and Aryl Aldehydes (共著) Tetrahedron ...
"Oligomers of aziridines and N-beta-aziridinoethylamides" Bull. of the Acad. of Sci. of USSR 37(11 part2): 2315-2323 (1988)... ... The method according to claim 1, wherein the moiety is an aziridine.. 17. The method according to claim 1, wherein the blood ... The method according to claim 21, wherein the moiety is an aziridine.. 37. The method according to claim 21, wherein the blood ... The method according to claim 41, wherein the moiety is an aziridine.. 56. The method according to claim 41, wherein the blood ...
where to buy 71243-81-7(Hexanedioic acid, polymer with N-(2-aminoethyl)-1,2-ethanediamine and aziridine, reaction products with ... 2-ethanediamine and aziridine, reaction products with epichlorohydrin and polyethylene glycol) including MSDS sheet(poisoning, ... 2-ethanediamine and aziridine, reaction products with epichlorohydrin and polyethylene glycol) for price inquiry. ... Hexanedioic acid, polymer with N-(2-aminoethyl)-1,2-ethanediamine and aziridine, reaction products with epichlorohydrin and ...
Comprehensive supplier list for Aziridine, 1-(1,1-dimethylethoxy)-2,2,3-trimethyl-,Aziridine, 1-(1,1-dimethylethyl)-2,3- ... Aziridine,1-(3-pyridinylcarbonyl)- (9CI); Aziridine, 1-nicotinoyl- (8CI);1-(3-Pyridinecarbonyl)aziridine Molecular Formula: C8H ... AZIRIDINE, 1-(1-PROPENYL)-, (E)- (6 suppliers). IUPAC Name: 1-[(E)-prop-1-enyl]aziridine , CAS Registry Number: 80839-91-4. ... AZIRIDINE, 1-(1-CYCLOHEXEN-1-YL)- (7 suppliers). IUPAC Name: 1-(cyclohexen-1-yl)aziridine , CAS Registry Number: 153616-85-4. ...
However, ring opening was found to be only feasible for the epoxide and the activated aziridine, and not for the nonactivated ... However, ring opening was found to be only feasible for the epoxide and the activated aziridine, and not for the nonactivated ... CHIRAL AZIRIDINES, FREE-ENERGY. journal title JOURNAL OF ORGANIC CHEMISTRY. J. Org. Chem.. volume. 76. issue. 21. pages. 8698 ... 2011). Reactivity of activated versus nonactivated 2-(bromomethyl)aziridines with respect to sodium methoxide: a combined ...
Vervisch K, Dhooghe M, Törnroos K, De Kimpe N. Synthesis of stereodefined piperidines from aziridines and their transformation ... Vervisch, K., Dhooghe, M., Törnroos, K., & De Kimpe, N. (2010). Synthesis of stereodefined piperidines from aziridines and ... AZIRIDINES. journal title JOURNAL OF ORGANIC CHEMISTRY. J. Org. Chem.. volume. 75. issue. 22. pages. 7734 - 7744. Web of ... Synthesis of stereodefined piperidines from aziridines and their transformation into conformationally constrained amino acids, ...
a Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type ... Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type ... Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type ... "Asymmetric Synthesis of Α,β-diamino Acid Derivatives with an Aziridine-, Azetidine- and Γ-lactone-skeleton via Mannich-type ...
... aziridine) Ligands. Together they form a unique fingerprint. * aziridine Chemical Compounds ... Enantioselective Addition of Organolithium Reagents to Imines Mediated by C2-Symmetric Bis(aziridine) Ligands. In: Tetrahedron ... Enantioselective Addition of Organolithium Reagents to Imines Mediated by C2-Symmetric Bis(aziridine) Ligands. / Johansson, F. ... Enantioselective Addition of Organolithium Reagents to Imines Mediated by C2-Symmetric Bis(aziridine) Ligands. Tetrahedron. ...
This project presents the progress towards regioselective nucleophilic ring openings on aziridines using p-methoxy phenol in ... This project presents the progress towards regioselective nucleophilic ring openings on aziridines using p-methoxy phenol in ... This project presents the progress towards regioselective nucleophilic ring openings on aziridines using p-methoxy phenol in ...
This search was done on November 16, 2018. It was compiled from government data last released on April 30, 2018. The data were obtained from the U.S. EPAs Risk Management System database (RMP).. ...
Zhou, J., Yeung, Y.-Y. (2014-04-18). N -bromosuccinimide-induced aminocyclization-aziridine ring-expansion cascade: An ... A novel N-bromosuccinimide induced aminocyclization-aziridine ring expansion cascade is reported. Substituted azepanes were ... N -bromosuccinimide-induced aminocyclization-aziridine ring-expansion cascade: An asymmetric and highly stereoselective ...
... ... Also covered, is manufacturers data on listed Global and China Aziridine Market production capacity, market share, production ... The influence of Aziridine industry policy is discussed in this research along with product specifications, manufacturing ... Statistics of global and Chinas key Aziridine manufacturers with their capacity of production, cost, price, profit, production ...
The reactive intermediates generated by laser flash photolysis (lambda(exc) = 248 or 193 nm) of the aziridines (E)-1-butyl-2,3- ... Gaebert C, Siegner C, Mattay J, Toubartz M, Steenken S. Laser flash photolysis of aziridines. Spectroscopic and kinetic ... Gaebert, C, Siegner, C, Mattay, Jochen, Toubartz, M, and Steenken, S. "Laser flash photolysis of aziridines. Spectroscopic and ... Gaebert, C., Siegner, C., Mattay, J., Toubartz, M., Steenken, S.: Laser flash photolysis of aziridines. Spectroscopic and ...
In addition to descriptions of the physical nature of aziridines, especially those features which underpin their utility as ... reactions and utility of aziridines exists; this review briefly summarizes the similarities and differences between oxiranes ... Aziridines, the nitrogenous analogues of epoxides, have until recently excited far less interest amongst synthetic organic ... and their nitrogenated analogues, concentrating on the underlying properties of aziridines and recent developments in their ...

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