method for the preparation of a pharmaceutical prepa - comb, affecting the central nervous system on the basis of benzodiazepine derivatives.and a working method for preparation of benzo - diazepinederivaten used here.

摘要

1336744 Substituted 2-amino-5-phenyl-3H- 1,4-benzodiazepine derivatives TAKEDA YAKUHIN KOGYO KK 16 Nov 1970 [15 Nov 1969] 32303/73 Divided out of 1336743 Heading C2C Novel compounds of the Formulµ IV and V wherein R is alkyl, aryl or amlkyl in which the aromatic ring of the aryl or aralkyl group is unsubstituted or substituted by one or more C 1-3 alkyl, C 2-4 alkenyl, C 1-3 alkoxy, C 2-7 acylamino, halo or nitro; RSP1/SP is hydrogen, C 1-6 alkyl, R 1 is C 1-3 alkyl; the rings A and/or B are unsubstituted or substituted by one or more halogen, nitro, trifluoromethyl, alkyl or alkoxy and the nitrogen at the 4-position is optionally linked to an oxygen atom may be prepared by reacting an amine II: with an ortho ester R-C(OR 1 ) 3 to form a compound IV and optionally reacting this product with ammonia to form a compound V and after each step, for products carrying an N-oxide optionally deoxygenating IV or V. Pharmaceutical compositions of IV and V show muscle relaxant, anti-convulsant, tranquillizing and sleep-inducing activity when administered orally or parenterally with the usual excipients.