PROCESS FOR PREPARING A PHARMACEUTICAL OR VETERINARY PREPARATION WITH SEDATIVE AND / OR MUSCLE-RELAXING ACTION BASED ON A 1-SUBSTITUTED-6- -PENYL-4H-S-TRIAZOLOŸ4,3, -AŸŸ1,4Ÿ-SUBVODASAPINE OBJECTED PREPARED PREPARATION AND METHOD FOR PREPARING A COMPOUND SUITABLE FOR USE IN THE FOREGOING PROCESS.

摘要

1331419 Triazolo-benzodiazepine derivatives UPJOHN CO 29 March 1972 [28 April 1971] 14878/72 Heading C2C Novel compounds of the Formula VI wherein R is chloro, bromo, cyano, C 1-3 alkoxy, di-(C 1-3 alkyl) amino, pyrrolidino, piperidino or morpholino; R 1 is hydrogen or C 1-3 alkyl; R 2 , R 3 , R 4 and R 5 are hydrogen, C 1-3 alkyl, fluoro, chloro, bromo, nitro, cyano, trifluoromethyl or C 1-3 alkoxy, alkylthio, alkylsulphinyl or alkylsulphanyl and salts thereof may be prepared (a) where R is chloro or bromo by reacting the 1-unsubstituted compound with N-chloro or N-bromo-succinimide; (b) where R is cyano, by reacting the 1-bromo compound with cuprous cyanide; and (c) where R is C 1-3 alkoxy or di- (C 1-3 alkyl) amino, pyrrolidino, piperidino or morpholine, by reacting the products of (a) with sodium or potassium C 1-3 alkoxide in C 1-3 alkanol or with the appropriate amine respectively. The intermediates of the Formula I may be prepared by reacting the appropriate 1,3 - dihydro - 5 - phenyl - 2H - 1,4 - benzodiazepine - 2 - thiones with formic acid hydrazide. Pharmaceutical compositions of the compounds VI show sedative, tranquilizing and muscle relazant activity when administered orally, parenterally or rectally with the usua 1 excipients.