摘要 |
1,161,270. Indole derivatives; phenylhydrazine sulphonic acid derivatives. MERCK & CO. Inc. 6 Oct., 1967 [13 Oct., 1966; 14 Aug., 1967], No. 45843/67. Heading C2C. Novel phenylhydrazine sulphonic acid derivatives of the general formula wherein R 3 is hydrogen, an alkali metal or an equivalent of an alkaline earth metal, an ammonium group or an ammonium group having up to four organic residues attached to the nitrogen atom and X is a dimethylamino or methoxy group, are prepared by acylation of a phenylhydrazine sulphonate of the general formula with a p-chlorobenzoyl halide or an azide, anhydride or nitrophenyl ester of p-chlorobenzoic acid. The phenylhydrazine sulphonic acid derivatives of the first general formula above may be converted to 1-p-chlorobenzoyl-2-methyl-5-(methoxy or dimethylamino) - 3 - indolylacetic acid by reaction with levulinic acid or an ester thereof. Pharmaceutical compositions having antiinflammatory activity comprise, as active ingredient, 1 - p - chlorobenzoyl - 2 - methyl - 5- (methoxy or dimethylamino) - 3 - indolylacetic acid, when prepared as described above, and an inert diluent, carrier or coating. |