1-Benzoyl-2-methyl-indole derivs. - with analgesic, antiinflammatory and antirheumatic activity prepd. by cyclising phenyl-hydrazine cpds. with ketone cpds.

摘要

In a process for the prodn. of new indoles of formula (Ie, a phenylhydrazine deriv. of formula (IIe is cyclised with a ketone of formula CH3-CO-CH2R2 (IIIe. In the formula R1 is halogen, H or OCH3; R2 is benzoyl, p-methylbenzoyl, p-methooxybenzoyl, 2,4-dimethoxybenzoyl, 3,4-dimethylbenzoyl, p-halobenzoyl, 2-methyl-4-nitroimidazolyl, 2-napthhoyl, methyl, or -CH2COOH; and R3 is p-methoxybenzoyl, 3,5-dinitrobenzoyl or, when Ri is other than -CH2COOH, p-halobenzoyl. (I) are analgesics, antiinflammatories and antirheumatic agents with fewer undesired side -effects (esp. ulcerogenicity) than known cpds. such as indomethacin. A specific cpd. is 1-(p-chlorobenzoyl)-2-methyl-3-benzoyl-5-methoxy indole.