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

✍ Scribed by O. Mansour; B. Szymonski; J. M. Morand; M. Cussac; F. Thomasson

• Book ID: 102345170
• Publisher: Journal of Heterocyclic Chemistry
• Year: 2001
• Tongue: English
• Weight: 38 KB
• Volume: 38
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570380315

✦ Synopsis

Abstract

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).