| 摘要 |
1323325 Indolo[1,2-d][1,4]benzodiazepin-6- ones A H ROBINS CO Inc 8 Oct 1970 [22 Oct 1969] 47911/70 Heading C2C Novel indolo[1,2-d][1,4]benzodiazepin-6-ones of the general formula wherein R is a hydrogen atom or a 1,2-dihydroxyethyl, hydroxy, C 1-8 alkylamino, di-C 1-8 -alkylamino, N-phenylcarbamoyloxy or N,N-diphenylcarbamoyloxy group ("phenyl" meaning an optionally monosubstituted phenyl group, the substituent being a C 1-8 alkyl, C 1-8 alkoxy or trifluoromethyl group or a fluorine, chlorine or bromine atom); R<SP>1</SP> is a hydrogen, chlorine or bromine atom or a C 1-8 alkyl, C 1-8 alkoxy or trifluoromethyl group; and n is 0, 1, 2, 3 or 4; and acid addition salts of those compounds which are basic are prepared (a) when n is 0 and R is a hydrogen atom, by reaction of a 2-(2- haloacetamidophenyl)-indole wherein X is a halogen atom, with an alkali metal hydride; (b) when R is other than a hydrogen atom, by reaction of the product of (a) with an alkali metal hydride followed by a halide of the general formula R(CH 2 ) n X; and (c) when R is an N-phenylcarbamoyloxy or N,N-diphenylcarbamoyloxy group, by reaction of the corresponding compound wherein R is a hydroxy group with a suitable phenyl isocyanate or carbamoyl chloride; followed optionally, where appropriate, by salification of the product. 2-(2-Haloacetamidophenyl)-indoles of the second general formula above are prepared by reaction of the phenylhydrazone of a 2-aminoacetophenone and polyphosphoric acid and reaction of the resulting 2-(2-aminophenyl)- indole with a haloacetyl halide. Pharmaceutical compositions having antidepressant and anticonvulsant activity comprise as active ingredient, an indolo[1,2-d][1,4] benzodiazepin-6-one of the first general formula above or a pharmaceutically acceptable acid addition salt of such a compound which is basic, together with a pharmaceutically acceptable carrier, and may be administered orally or parenterally.
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