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Peter A. Crooks Trevor Deeks Francesco Desimone 《Journal of heterocyclic chemistry》1989,26(4):1113-1117
A series of 5-benzoyl-5-phenyl- and S-phenyl-5-phenylhydroxymethylhydantoins have been synthesized from the reaction of urea, N-monosubstituted ureas and sym-N-N-disubstituted ureas with phenyltriketone hydrate, via a pinacol-pinacolone-type rearrangement mechanism. The compounds were evaluated for anti-convulsant activity in mice. 相似文献
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L. A. Sviridova S. V. Afanas'eva K. N. Zelenin G. A. Golubeva I. P. Bezhan Yu. G. Bundel' 《Chemistry of Heterocyclic Compounds》1987,23(4):403-406
1-Acyl-5-hydroxypyrazolidines readily exchange their hydroxyl group when treated with primary amines or alcohols to form the corresponding 5-amino or 5-alkoxypyrazolidines. An acid catalyst is needed for the preparaton of the 5-alkoxypyrazolidines.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 484–487, April, 1987. 相似文献
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Na5Nb05 and Na5Ta05 Phases. Crystal Structure of Na5NbO5 New ternary oxides of formulas Na5NbO5 and Na5TaO5 have been prepared. They crystallize in the monoclinic system (space group C2/c). The crystal structure of Na5NbO5 has been determined. It derives from a NaCl-type structure by ordering of the cations and of the oxygen vacancies in the anionic sublattice, the corresponding formula being Na5/6Nb1/6O5/6□1/6. Sodium and niobium have a distorted square-pyramidal surrounding. 相似文献
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Fabian Fischer Daniel Berger Markus Neuenschwander 《Angewandte Chemie (International ed. in English)》1998,37(15):2138-2140
Strong nucleophiles are needed for inducing ring opening 3 → 4 since the pyrylium salt intermediates 3 , formed from 5-X-substituted 5-aminopenta-2,4-dienals 2 upon treatment with acid, are quite unreactive due to “aromatic” stabilization. However, this allows an easy access to a variety of 2-aminopyrylium salts 3 from “push–pull” enynes 1 . X=OAc, F, Cl, Br, I, OPh. 相似文献
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James R. Piper Balakrishnan Ramamurthy Cheryl A. Johnson Joseph A. Maddry Glenys M. Otter Francis M. Sirotnak 《Journal of heterocyclic chemistry》1995,32(4):1205-1212
5-Propyl-5-deaza and 5-butyl-5-deaza analogues of classical antifolates were synthesized by extensions of a previously reported general route which proceeds through 2,4-diamino-5-alkylpyrido[2,3-d]pyrimidine-6-carbonitrile intermediates followed by reductive condensation with diethyl N-4-(aminobenzoyl)-L-glutarnate to give diethyl esters of 5-alkyl-5-deazaaminopterin types. N10-Methyl derivatives, i.e., derivatives of 5-alkyl-5-deazamethotrexate, were also prepared by reductive methylation of the N10-H compounds. 5-Ethyl-5-deazamethotrexate was prepared using an alternative route through 6-(bromomethyl)-2,4-diamino-5-ethylpyrido[2,3-d]pyrimidine. These antifolates were evaluated for inhibition of dihydrofolate reductase (DHFR) from L1210 cells, their effect on L1210 and S180 tumor cell growth in culture, and carrier-mediated transport through L1210 cell membranes. Inhibitory effect on DHFR was lowered relative to methotrexate in 5-propyl-5-deazaaminopterin and 5-propyl-5-deazamethotrexate by 2- to 3-fold (Ki = 9.3 and 11.7 pM, respectively, vs. 4.3 pM for methotrexate) and by 17- to 18-fold in 5-butyl-5-deaza-aminopterin and 5-butyl-5-deazamethotrexate (Ki = 74 and 78 pM, respectively). Molecular modeling using graphics derived from human DHFR show the propyl and butyl compounds interacting with the enzyme in conformations that account for these slight decreases in binding. 相似文献
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Zusammenfassung 5-Methylthiouracil wird auf verschiedenen Wegen durch Ringschlußreaktionen von Formylmethylthioessigester bzw. Derivaten mit S-Methylisothioharnstoff oder Thioharnstoff und Hydrolyse des primär gebildeten 2,5-Di-(methylthio)-4-oxypyrimidins bzw. 5-Methylthio-thiouracils dargestellt.Oxydation mit Peressigsäure führt zu 5-Methylsulfinyl- und 5-Methylsulfonyluracil. 5-Methylsulfonyluracil kann auch durch Oxydation von 2,5-Di-(methylthio)-4-oxypyrimidin und 5-Methylthio-thiouracil gewonnen werden.Herrn Prof. Dr.F. Wessely in freundschaftlicher Verehrung zu seinem 70. Geburtstag gewidmet. 相似文献
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Seiko Nan'ya Etur Maekawa Wen-Bing Kang Yoshio Ueno 《Journal of heterocyclic chemistry》1986,23(6):1697-1700
The 1,6-disubstituted- and 4,6-disubstituted-11-aza-5H-benzo[a]phenoxazin-5-one as well as 6-substituted-11-aza-5H-pyrido[a]phenoxazin-5-one derivatives were prepared by the condensation of 2-amino-3-hydroxypyridine with 5-substituted-2,3-dihalogeno-1,4-naphthoquinones and 6,7-dibromo-5,8-quinolinequinone respectively. The resulting compounds were subjected to reduction, acetylation, dehalogenation and reaction with aniline. 相似文献
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S. Nakhar I. G. Tishchenko O. N. Bubel' V. I. Biba 《Chemistry of Heterocyclic Compounds》1987,23(7):809-812
Mixtures of stereoisomeric 2-diethoxymethyl-5-ethyloxazolidines with one of the stereoisomeric forms predominating were obtained by the reaction of 2-ethyl-2-formyloxirane diethyl acetal with alkyl-substituted Schiff bases in ethanol solution.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, 985–988, July, 1987. 相似文献
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H. Preiss 《无机化学与普通化学杂志》1971,380(1):56-64
Crystals of PCl5NbCl5 and PCl5TaCl5 are isomorphous; space group P1 . The structures are ionic, consisting of tetrahedral cations PCl4+ and octahedral anions NbCl6? and TaCl6?, respectively. Twinning is frequently observed in both compounds; an explanation thereof is given on the basis of the OD theorie. 相似文献
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