| 摘要 |
<p>1,248,225. 15#,16#- Methylene steroids. SCHERING A.G. 15 Oct., 1968 [20 Oct., 1967], No. 48873/68. Heading C2U. Novel steroids of the formula (in which R 1 is H or acyl and R 2 is H, alkyl, alkenyl or alkynyl) are prepared by reducing by the Birch method or electrolytically steroids of the formula (wherein X is alkyl or tetrahydropyranyl and R 3 is H or C 1-4 alkyl) and hydrolysing with a strong acid the resulting #<SP>2</SP>'<SP>5(10)</SP>-3-ethers to give the required products wherein R 1 is H and R 2 is H or alkyl. These may, when required, be converted to 17-acylates, or, possibly after protection of the 3-keto group, oxidized to the 17-ones and these alkylated, alkenylated or alkynylated at position-17 in known manner to give the 17a-hydrocarbyl-17#-ols. In these an alkynyl group can be reduced to an alkenyl or alkyl group and a 17#-OH group may be acylated. 3 - Methoxy - 18 - methyl - 15#,16# - methylene- #<SP>1,3,5(10)</SP> - estratrien - 17# - ol is prepared from 3 - methoxy - 18 - methyl - #<SP>1,3,5(10)</SP> - estratrien- 17-one 17-ethylene ketal (from the free 17-one) via the 16α-bromo-derivative, the 15-dehydro- 16- unsubstituted derivative, the corresponding free 17-one, and 3-methoxy-18-methyl-15#,16#-methyl. ene-#<SP>1,3,5(10)</SP>-estratien-17-one. The steroids of the invention are anabolic agents and may be made up into pharmaceutical compositions with suitable carriers.</p> |
