CERTAIN 9 -(CHLORO OR FLRUORO)-16( OR )-METHYL-11 ,17 -DIHYDROXYPREGNA-1,4-DIENE-3,20-DIONE 17 -ACYLATES OR 11 ,17 -DIACYLATES AND CERTAIN PREPARATURE PROCESSES

摘要

1510617 21 - Deoxy - 16 - methyl corticosteroid derivatives PLURICHEMIE ANSTALT 26 March 1975 [27 March 1974 (2) 10 May 1975] 12608/75 Heading C2U The invention comprises compounds of formula wherein X is Cl or F, and either (i) R 1 is OH or C 1-16 acyloxy and R 2 is tetrahydropyran-2-yloxy, or (ii) R 1 is C 6-16 acyloxy and R 2 is OH, or (iii) R 1 and R 2 are each C 1-16 acyloxy. Preparation of I is from the corresponding 11, 17-diols by conversion to their 11-(tetrahydropyran-2-yl) ethers or 11-(di- or tri-chloro- or fluoro-acetates), followed as appropriate by 17-esterification, selective 11-hydrolysis (or solvolysis in the presence of silica gel) and 11- esterification. 21 - Deoxybeclomethasone and its 16- epimer are prepared from their 9,11-epoxy analogues by reaction with HCl. 21 - Deoxybeclomethasone 11 - propionate is prepared from its 11-(tetrahydropyran-2-yloxy) analogue by reaction with EtCO 2 H. Anti-inflammatory compositions for oral, topical and parenteral administration comprise a compound I and a carrier.