CONVENIENT SYNTHESIS OF S-FLUOROMETHYL 6ALPHA, 9ALPHA-DIFLUORO-11BETA-HYDROXY-16ALPHA- METHYL-17ALPHA-PROPIONYLOXY-3-OXOANDROSTA-1, 4-DIENE-17BETA-CARBOTHIOATE

摘要

The present invention provides a convenient process for the preparation of S-fluoromethyl 6alpha,9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionyloxy-3-oxoandrosta-1,4-diene-17beta-carbothioate, a compound of formula 1, comprising (a) treating 17beta-[(N,N-dimethylcarbamoyl)thio]carbonyl-6alpha,9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionyloxy-3-oxoandrosta-1,4-diene, a compound of formula 3 with alkali metal carbonate-alcohol system to obtain 6alpha,9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionyloxy-3-oxoandrosta-1,4-diene-17beta-carbothioic acid, a compound of formula 4; (b) reacting the compound of formula 4 with bromofluoromethane to yield the compound of formula 1.