| 摘要 |
1,229,428. 1,2-Methylene-steroids. SCHERING A.G. 1 April, 1968 [31 March, 1967; 11 Jan., 1968], No. 15526/68. Heading C2U. 17 - Hydroxy - 6#,7# - epoxy - 1α,2α - methylene-4-pregnene-3,20-dione and acylates thereof, which are novel compounds, are prepared by reacting 17-acyloxy-6#-(acyloxy or hydroxy)- 7α-(chloro or bromo) -1α,2α-methylene-4-pregnene-3,20-diones with a base in an inert solvent, and, if desired, when the product is a free 17-ol, acylating this. The starting materials are prepared from the corresponding #<SP>6</SP>-steroids; reaction of these with N-bromo- or N-chloro-succinimide and water in the presence of perchloric acid in dioxan gives the 6#-hydroxy-7#-halogeno-steroids, while reaction with the same halogenating agents and a carboxylic acid in tetrahydrofuran saturated with HCl gives the 6#-acyloxy-7α- halogeno-steroids. The novel steroids are stated to have strong gestagenic activity with little anti-androgenic effect and no ovulation inhibiting effect, and they may be made up into pharmaceutical compositions with suitable carriers. |
