Bendodiazocine derivatives and process of making the same

US4243585A · 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: Jan 23, 1978
• Grant date: Jan 6, 1981
• Expiry date: Jan 23, 1998

Classification

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

Abstract

1,2,3,4-Tetrahydro-1,5-benzodiazocines having the following formula ##STR1## in which R.sup.1 is a hydrogen, alkyl radical having at most 6 carbon atoms, methoxyethyl, or benzyl radical, PA1 R.sup.2 is a halo, hydroxyl, acetoxy or benzoxy radical, PA1 R.sup.3 is a phenyl, 2-methylphenyl, 2-chlorophenyl, 2-bromophenyl, 2-fluorophenyl, 2-nitrophenyl, 2-(trifluoromethyl)phenyl, 3-(trifluoromethyl)phenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,4-dimethoxyphenyl, or 3,4,5-trimethoxyphenyl radical, PA1 R.sup.4 is a hydrogen, chloro, fluoro, bromo, trifluoromethyl, methyl, methoxy, or methylthio radical, and PA1 R.sup.5 is a hydrogen or methoxy radical, or R.sup.4 and R.sup.5 together are an ethylendioxy radical, or an acid addition salt of the said benzodiazocine, and processes of making the same are described. The benzodiazocines are tranquilizing agents and starting compounds for the production of benzodiazepines which are also useful as tranquilizing agents as well as anticonvulsive, sedative, and muscle-relaxing agents.