| 摘要 |
1377993 6α,16α - Dimethyl - #<SP>1,4</SP> - pregnadienes SCHERING AG 22 Nov 1971 [28 Nov 1970] 54050/71 Heading C2U Novel steroids of the formula (wherein R is H or acyl, X is F, Cl or Br, and Y is #-halogenomethylene the halogen atom of which has an atomic weight equal to or smaller than that of X, or Y is #-hydroxymethylene or carbonyl) are prepared from corresponding #<SP>9(11)</SP>-steroids or their #<SP>4</SP>-analogues by adding 2 halogen atoms or HOCl or HOBr across the 9(11)-double bond followed when required by (a) conversion of a 9α-bromo- or chloro-11#-ol to a 9,11#-epoxide and conversion of this to a 9α - fluoro- or chloro - 11# - ol; (b) microbiological #<SP>1</SP>-dehydrogenation; (c) oxidation of an 11#-ol to an 11-one; (d) hydrolysis of a 21- acylate to a 21-ol; and/or (e) esterification of a 21-ol. #<SP>1</SP>-Dehydrogenation may for example be effected with Bacillus lentus or Arthrobacter simplex. 21 - Acetoxy - 6α,16α - dimethyl - #<SP>1,4,9(11)</SP>- pregnatriene - 3,20 - dione is prepared by converting 11α - hydroxy - 21 - acetoxy - 6α,16α- dimethyl - #<SP>1,4</SP> - pregnadiene - 3,20 - dione (prepared by acetylation of the corresponding 21-ol) to 11α-mesyloxy-21-acetoxy-6α,16α- dimethyl - #<SP>1,4</SP> - pregnadiene - 3,20 - dione and then heating this with glacial acetic acid and sodium acetate. 21-Acetoxy-6α,16α-dimethyl - #<SP>4,9(11)</SP> - pregnadiene - 3,20 - dione is prepared by heating 11#-hydroxy-21-acetoxy- 6α,16α - dimethyl - #<SP>4</SP> - pregnene - 3,20 - dione with pyridine, DMF and methanesulphonyl chloride. The novel steroids are stated to be antiphlogistic agents with a lesser thymolytic side effect than comparable known steroids. They may be made up into pharmaceutical compositions with suitable carriers. Reference has been directed by the Comptroller to Specification 990,384. |
