Process of making benzodiazepine derivatives

US4595531A · kind A · utility

Assignee

• Kali-Chemie Aktiengesellschaft · DE

Inventors

• Wolfgang Milkowski
• Renke Budden · Hannover, DE
• Siegfried Funke
• Rolf Huschens · Hannover, DE
• Hans Liepmann · Hannover, DE
• Werner Stuhmer
• Horst Zeugner

Key dates

• Filing date: Apr 24, 1984
• Grant date: Jun 17, 1986
• Expiry date: Apr 24, 2004

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Benzodiazocines corresponding to the formula ##STR1## are converted to benzodiazepines corresponding to the formula ##STR2## of claim 1 by subjecting the benzodiazocine (a) if it is halogen-substituted in the 3-position to a thermal treatment which may also take place in the presence of a nucleophilic agent for the reaction or (b) if the 3-position is hydroxy substituted to treatment with a Lewis acid which is a chlorinating or brominating agent. Whenever the diazepine obtained as the final product has a 2-halogenomethyl group it may then be converted to benzodiazepine which is otherwise substituted in the 2-position.