| 摘要 |
The invention comprises 6a -methyl-9a -fluoro-16-methylene - 11 - keto - 17a - hydroxy (and acetoxy) - progesterone, 6a - methyl - 9a -fluoro - 16 - methylene - 11b ,17a - dihydroxy -1 - dehydro - progesterone, and 6a - methyl - 16-methylene-cortisone, -hydrocortisone, -prednisone, and -prednisolone and the 9a -fluoro derivatives thereof, and a process for the preparation of steroids of the general formula <FORM:0987064/C2/1> wherein R1 represents H,H; a H,b OH; or O; R2 represents H, OH or acyloxy; R3 represents H or acyl; and Y represents hydrogen or fluorine, by treating steroids of the general formula <FORM:0987064/C2/2> wherein R1, R2, R3 and Y have the above significance, with hydrogen in the presence of a noble metal catalyst such as palladium or platinum, if desired, on a carrier. The above process may be extended in that the 4-pregnene product is converted to a 1,4-pregnadiene, e.g. by treatment with the microorganisms Corynebacterium simplex or Bacillus sphaericus. In the products prepared by the above processes, hydroxy groups in the 17- and/or 21-position may be acylated, e.g. with a carboxylic, sulphuric or phosphoric acid, acyloxy groups in the 17- and/or 21-positions may be hydrolysed, and an 11-hydroxy group may be oxidized to an 11-keto group. Therapeutic compositions contain as the active ingredient a steroid of the first general formula above. The compositions have a gestogenic activity and may be in the form of tablets, pills, dragees, emulsions, solutions, injectable solutions or sprays. Steroids of the second general formula above are prepared by treating the corresponding 3-enol ether, 3-enol acylate or 3-ethylene ketol with tetrabromomethane in the presence of collidine and then hydrochloric acid. Specification 880,464 is referred to. Reference has been directed by the Comptroller to Specification 858,033. |
