BENZOPHENONE DERIVATIVES AND THEIR PRODUCTION

摘要

1441357 Substituted amido-benzophenones CASSELLA FARBWERKE MAINKUR AG 6 Nov 1974 [10 Nov 1973] 47993/74 Addition to 1377312 Heading C2C The invention comprises compounds of the Formula (I) and acid addition salts thereof, wherein A is an unsubstituted or substituted ortho-phenylene radical, B is an unsubstituted or substituted phenyl radical, R 1 and R 2 are each H or C 1 -C 4 alkyl or alkenyl, R 3 is -COOC 3 H 7 , -COOC 4 H 9 with the exception of t-butoxycarbonyl when m is zero, -COOPh, Ph or -(CY)NHR 4 wherein Y is -O- or -S- and R 4 is phenyl or C 1 -C 4 aliphatic radical, n is 1 or 2 and m is 0, 1, 2, or 3, and when m is zero R 3 can also be -COOCH 3 or -COOC 2 H 5 . They may be obtained by (a) reacting a benzophenone derivative of the formula B-CO-A-NR 1 -CO-C n H 2n -X (II) with a compound of the formula Y1-C m H 2m -R 3 wherein one of X and Y1 is NHR 2 and the other is halogen; (b) when m is 2 or 3, reacting a benzophenone derivative of Formula II with a compound of the formula: C m H 2m-1 R 3 which contains an aliphatic double bond and wherein m is 2 or 3; (c) when R 3 is (CY)NHR 4 and m is O, reacting a benzophenone derivative of the formula with a compound of the formula: R 4 NCY or (d) when R 3 is (CO)NHR 4 , reacting a benzophenone derivative of the formula: wherein R 5 is alkyl or aryl, with an amine of the formula R 4 NH 2 . Compounds of Formula I have a depressant action on the central nervous system. Some of these compounds also possess muscle-relaxing and aggression-inhibiting properties. They may be administered as tablets, suppositories, capsules, emulsions or suspensions or in conjunction with other therapeutically active substances.