9.,11.beta.-substituted and 11.beta.-substituted estranes

Details 9.,11.beta.-substituted and 11.beta.-substituted estranes 9.,11.beta.-substituted and 11.beta.-substituted estranes

C - Chemistry, Metallurgy

07

J

167/192, 260/31,

C07J 1/00 (2006.01) C07J 7/00 (2006.01) C07J 11/00 (2006.01) C07J 17/00 (2006.01) C07J 41/00 (2006.01) C07J 51/00 (2006.01)

Patent

CA 1317932

Abstract of the Disclosure 9.alpha.,11.beta. and 11.beta.-substituted estranes are disclosed which have the general formula: Image wherein R1 is hydrogen, a lower alkyl or cycloalkyl or a lower acyl; R2 is a nitrate, a halo, a lower alkyl or a hydroxyl; R3 is hydrogen, hydroxyl or a lower alkoxy; R4 is either a carbonyl oxygen or is a pair of groups, the alpha position one of which is hydrogen or a lower alkynyl and the beta one of which is hydroxyl, a lower alkyl or a N alkanoic acid ester; and R5 is hydrogen or a lower alkyl. When R2 is nitrate, R3 is hydroxyl, and R4 is carbonyl, R5 must be a lower alkyl. When R2 is a halo R3 must be hydrogen. When R2 is hydroxyl R5 must be a lower alkyl. The compounds of the invention exhibit estrogenic activity and postcoital contraceptive activity. A process for their manufacture and their use in pharmaceuticals is also disclosed.

517374

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