| 摘要 |
1,232,348. Benzoxazepinones. CIBA-GEIGY A.G. 18 March, 1969 [21 March, 1968; 19 Feb., 1969], No. 14090/69. Heading C2C. Novel benzoxazepinones of Formula I in which Ph is an o-phenylene radical which may be substituted, e.g. by halogen atoms or nitro groups, Ph<SP>1</SP> is an aryl radical, e.g. a phenyl or halophenyl radical, R is a tertiary aminoalkyl radical in which the amino nitrogen atom is separated from the cyclic nitrogen atom by at least two carbon atoms, and R<SP>1</SP> is a hydrogen atom or an alkyl group, and acid addition salts thereof, are prepared by reacting a compound of Formula II with a compound of formula R-X, in which X is a reactive esterified hydroxy group separated from R by at least two carbon atoms. The free bases of Formula I and their acid addition salts may be interconverted. Starting materials of Formula II are prepared by cyclization of 2-(2-oxoethoxy)-benzamides of Formula III which are themselves obtained by reacting a suitable α-halo-oxo compound with an appropriate salicylic acid amide. Pharmaceutical compositions having antiinflammatory, antiphlogistic, analgesic and psychopharmacological activity, for oral, topical or parenteral administration comprise a compound of Formula I or a therapeutically acceptable acid addition salt thereof, together with a pharmaceutically suitable carrier. |
