Synthesis of 3-carboxylic derivatives of 1,5-benzodiazepines

被引:2
|
作者
Mansour, O
Szymonski, B
Thomasson, F
Morand, JM
Cussac, M [1 ]
机构
[1] Univ Grenoble 1, Fac Pharm, CNRS,UMR 5063, Dept Pharmacochim Mol,Lab Chim Therapeut, F-38706 La Tronche, France
[2] Univ Grenoble 1, Fac Pharm, CNRS,UMR 5063, Dept Pharmacochim Mol,Serv Commun,RMN, F-38706 La Tronche, France
关键词
D O I
10.1002/jhet.5570380315
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of 3-carboxylic derivatives of disubstituted 1,5-benzodiazepines (5-9) was synthesized by heterocyclisation from 1,2-diaminobenzene (1) with dibenzoylmethane (2) followed by bromination on position 3 and by introduction of the carboxylic group or introduction of the malonic moiety. Reduction of the heterocycle gave the perhydro derivative diethyl (2,4-diphenyl-1,2,4,5-tetrahydro-3H-1,5-benzodiazepin-3-yl)malonate (9).
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页码:641 / 643
页数:3
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