Androstane carbothioates

Details Androstane carbothioates Androstane carbothioates

C - Chemistry, Metallurgy

07

J

260/15, 260/83

C07J 31/00 (2006.01) C07J 3/00 (2006.01) C07J 41/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 1201114

ABSTRACT Compounds of the formula Image (I) wherein R1 represents a fluoxo-, chloro- or bromo- methyl group or a 2'-fluoroethyl group, R2 represents 1 group COR6 where R6 is a C1-3 alkyl group or OR2 and R3 together form a 16.alpha.,17.alpha.-isopropylidene- dioxy group; R3 represents a hydrogen atom, a methyl group (which may be in either the .alpha.- or .beta.-configuration) or a methylene group; R4 represents a hydrogen, chlorine or fluorine atom; R5 represents a hydroqen or fluorine atom and symbol Image represents a single or double bond have good anti-inflammatory activity, particularly on topical applications. The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9.alpha.-halo-11.beta.- hydroxy grouping.

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