| 摘要 |
1424568 2,3-Dihydro-3-oxo-1,4-benzoxazines CERPHA 26 July 1973 [3 Aug 1972] 35662/73 Heading C2C Novel 2,3-dihydro-3-oxo-1,4-benzoxazines of the general formula wherein R 1 is a hydrogen atom or C 1-5 alkyl group, each of R 2 , R 3 and R 4 is a hydrogen or halogen atom or a nitro, C 1-5 alkyl, C 1-5 alkoxy or C 2-5 alkenyl group and R 5 is a hydrogen atom or acyl group, are prepared (a) by reacting an alkali metal salt of a compound of the general formula with a compound of the general formula wherein X is a halogen atom and Y is -OR 5 or X and Y together form an oxygen atom, (b) by reacting a compound of the general formula with a compound of the general formula R 1 -CHX-CO-A, wherein A is a chlorine atom or alkoxy group and X is a halogen atom, the reaction taking place in the presence of a base when A is an alkoxy group and a base being added after the release of HCl when A is a chlorine atom, or (c) when R 5 is an acyl group, by acylation of the corresponding compound in which R 5 is a hydrogen atom. Pharmaceutical compositions having analgesic and anti-oedema activity comprise, as active ingredient, a 2,3-dihydro-3-oxo-1,4-benzoxazine of the first general formula above, in association with a physiologically acceptable vehicle.
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