| 摘要 |
The invention comprises steroids of the formula <FORM:1028613/C2/1> wherein R is hydrogen or hydroxy, X is a -hydroxymethylene or b -hydroxymethylene, and Z is selected from <FORM:1028613/C2/2> and their preparation by microbiological 11-hydroxylation of the corresponding 11-unsubstituted steroids or their 21-acylates using a species of fungus of the order Mucorales, the genus Aspergillus or the species Curvularia lunata at pH of 7 to 9. A large number of species of fungus are referred to, but those preferred are of the family Mucoraceae or Cunninghamellaceae and of the genus Rhizopus, Absidia or Cunninghamella, the first two of these giving 11a -hydroxy-products and the last 11b -hydroxy-products. Aspergillus species also give 11a -hydroxy-products, and Curvularia lunata gives 11b -hydroxy-products. The invention also comprises a process for the preparation of the steroids of Formula I by treatment of the corresponding 3 - tosyloxy - D 5 - 6 - unsubstituted steroids with potassium acetate in an inert solvent. Examples are given. Steroids of the Formula I wherein X is an unsubstituted methylene group are prepared by converting the corresponding 3b -hydroxy-D 5-6-unsubstituted steroids to their 3-tosylates and heating these with potassium acetate in an inert solvent. The 3,5-cyclo-6b -hydroxy-steroids of the invention, which are stated to be sedatives, tranquilizers, muscle relaxants and analgetic c.n.s. system depressants, may be made up into pharmaceutical compositions with suitable carriers. These may take the form of tablets, powders, capsules, pills, solutions, suspensions, emulsions, syrups or elixirs.
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