(12 Alpha)-Hydroxy-(8 alpha)-oestradiols - prepd. by fermenting an (8alpha)-oestradiol with glomerella, used to treat women during menopause

摘要

12alpha-hydroxy-8alpha-oestradiols of formula (I) are new In (I) R1 is H, acyl, alkyl or cycloalkyl; and R2 and R3 are H or acyl). (I) shows a favourable oestrogen dissociation, in that they have a strong effect in the vagina and a weak effect in the uterus. (I) can therefore be used e.g. to treat women during the menopause. (I) are prepd. by fermenting an 8alpha-oestradiol of formula (I) where OR2 is replaced by H, with Glomerella (pref. Glomerella cingulata ATCC 12097) to introduce the 12alpha-OH gp., and then opt. etherifying and esterifying any free OH gps.