Premium
Synthesis of 3‐Carboxylic derivatives of 1,5‐benzodiazepines
Author(s) -
Mansour O.,
Szymonski B.,
Morand J. M.,
Cussac M.,
Thomasson F.
Publication year - 2001
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570380315
Subject(s) - chemistry , dibenzoylmethane , diethyl malonate , malonate , moiety , derivative (finance) , halogenation , malonic acid , medicinal chemistry , carboxylic acid , organic chemistry , catalysis , financial economics , economics
A series of 3‐carboxylic derivatives of disubstituted 1,5‐benzodiazepines (5–9) was synthesized by hetero‐cyclisation 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 hetero‐cycle gave the perhydro derivative diethyl (2,4‐diphenyl‐1,2,4,5‐tetrahydro‐3 H ‐1,5‐benzodiazepin‐3‐yl)malonate (9) .