7-Hydroxy-17-alpha-hydrocarbyl-oestradiol derivs - prepd by 17-alkylating 7-hydroxy-oestrone derivs

摘要

Oestradiol derivs. of formula (I) (where R1 is H, acyl, alkyl, cycloalkyl or an O-contg. satd. heterocyclic gp; R2 and R3 are H, acyl or an O-contg. satd. heterocyclic gp; and R4 is an opt. unsatd. lower hydrocarbon gp. which is unsatd. can be substd. by Cl; and OR2 can be in the alpha- or beta-posn) e.g. 17alpha-ethynyl-1,3,5(10)-oestratriene-3,7alpha,17beta-triol are new cpds. (I) are oestrogens with a favourably dissociated pharmacological action. they have a strong vaginotropic effect but a weak uterotropic effect and are therefore suitable for the treatment of oestrogen deficiency disorders (e.g. the postmenopausal syndrome in women) in which a centrally mediated effect on the uterus should be avoided but an effect on the vagina is desirable. (I) are also useful as inters. for other pharmacologically valuable steroids.