摘要 |
1282520 16-Methyl-pregnane compounds MERCK PATENT GmbH 22 Sept 1970 [15 Nov 1969] 45060/70 Heading C2U Novel steroids of the formula wherein OR is an esterified or etherified hydroxy group and R<SP>1</SP> is F, Cl, Br, CH 3 or CF 3 , and their novel #<SP>4,6</SP>-analogues, are prepared by esterification or etherification of the free 3-ols or reactive derivatives thereof or by solvolysis of corresponding steroids containing a functionally modified 20-keto group. The etherified hydroxy group is defined as one wherein R is C 1-12 alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, optionally substituted. 6α,16α - Dimethyl - 20,20 - ethylenedioxy - 4- pregnen-3#-ol is obtained by ketalizing the hydrochloride of 3-pyrrolidino-6,16α-dimethyl- 3,5-pregnadien-20-onewithethyleneglycol, alkaline splitting to form the 3-ketone and reduction with NaBH 4 . The novel steroids, which are stated to have gestagenic, anti-ovulatory, cycle-influencing, anti-androgenic, gonadotropin-influencing, antiestrogenic and anti-fertility activities, may be made up into pharmaceutical compositions with suitable carriers. |