| 摘要 |
1,268,424. Indolizine derivatives. BEECHAM GROUP Ltd. 18 Sept., 1970 [4 Oct., 1969], No. 48856/69. Heading C2C. The invention comprises compounds of formulae the pharmaceutically acceptable salts and esters of I, and the esters and salts of II, wherein R and R<SP>2</SP> are each C 1-6 alkyl, and R<SP>3</SP> is aryl or C 1-6 alkyl. These compounds are prepared by reacting 2-formylpyridine with Ph 3 P : CRCO 2 Et to give 2-(2-carbethoxyalk-1-enyl)pyridine, hydrogenating this (H 2 /Pd-C) to 2-(2-carbethoxyalkyl)pyridine, reacting with (e.g.) BrCH 2 Ac to give 1-acetonyl-2-(2-carbethoxyalkyl)pyridinium bromide which is treated with a base to give II, esterifying the latter and reacting the ester with a reactive derivative of R<SP>3</SP>CO 2 H, and optionally hydrolysing the ester of I thus obtained. Therapeutic compositions for oral or parenteral administration comprise compounds I (above), and their pharmaceutically acceptable salts and esters, which have analgesic and anti inflammatory activity. |
