STEROIDAL/16ALPHA,17-B/NAPHTALENO AND CYCLOHEXENE-21-CARBOXYLIC ACID ESTERS

摘要

Steroids having the formula IMAGE and esters thereof, wherein X is hydrogen or halogen; Y is hydrogen, methyl or fluorine; R4 is chlorine, fluorine or hydroxy and R5 is hydrogen or R4 and R5 together are =O; R2 and R3 are each hydrogen, alkyl, phenyl or phenyl substituted with one or more halogen alkyl or alkoxy groups, or R2 and R3 together with the double bond to which they are attached form a benzene ring; R6 and R7 are each hydrogen, alkyl, alkoxy, formyl, IMAGE phenyl or cyano and in addition hydroxy, halogen, carboalkoxy and alkylcarbonyl when R2 and R3 are separate, with the proviso that when R6 and R7 are different one of R6 and R7 is hydrogen; R8 is hydrogen or -CH(R9)(R10) wherein R9 and R10 are each hydrogen or alkyl, have anti- inflammatory activity. Preparation (i) from the corresponding 21-ols by oxidation via 20-one-21-als (and/or 21-acetals thereof) and/or 20-hydroxy-21-oic acids (and/or 21-esters thereof); or (ii) from the corresponding ???16-21-ols (lacking the fused ring) by oxidation as in process (i) followed by fusing the cyclohexene or tetrahydronaphthalene group into the 16,17-position.