7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharmaceuticals

US4505908A · kind A · utility

Assignee

• Kali-Chemie Pharma GmbH · DE

Inventors

• Horst Zeugner
• Michael Ruhland · Hannover, DE
• Hans Liepmann · Hannover, DE
• Wolfgang Milkowski
• Herbert Muesch · Wennigsen (Deister), DE

Key dates

• Filing date: Sep 23, 1982
• Grant date: Mar 19, 1985
• Expiry date: Sep 23, 2002

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D245/06
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are 7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines of the formula I ##STR1## in which R.sub.1 is a hydrogen atom or a lower alkoxy or alkanoyloxy radical and R.sub.2 is a halogen atom. The compounds possess psychopharmacological, and especially anti-aggressive properties. To manufacture compounds of formula I, corresponding 2-halomethyl-7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines are cyclized to corresponding 7-bromo-1,2-methylene-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines and in these the aziridine ring is opened through treatment with a lower alcohol or a lower carboxylic acid in the presence of a Lewis acid.