| 摘要 |
1,146,053. Steroids. UPJOHN CO. 6 April, 1966 [7 April, 1965], No. 15371/66. Heading C2U. The invention comprises a compound of the formula wherein R 1 and R 2 are H or CH 3 , Y<SP>1</SP> is C=O, in which n is 1 or 2 and R‹ is H or (C 1 -C 6 ) alkyl; Z is H or the acyl radical of a (C 1 -C 12 ) hydrocarbon carboxylic acid, and Q is H, (C 1 -C 12 ) alkyl; or -C#CA, -CH=CHA or -CH2CH 2 A, where A is H, (C 1 -C 12 ) alkyl, Cl, Br, or CF 3 ; except that when R 2 is H and Y<SP>1</SP> is C = O then Z can only be the acyl radical of a (C 1 -C 12 ) hydrocarbon carboxylic acid, and Q can only be -C#CX, where X is Cl or Br a process for the production of a compound wherein R 1 , Z and Q are as defined above, by methylation at the 2α-position, the corresponding 2-unsubstituted compound, a process for the production of compounds of the formulµ wherein Y is C = O, R 1 and R 2 are H or CH 3 , Z and A are as defined above except that when R 2 is H and Y is C = O, Z must be the acyl radical of a (C 1 -C 12 ) organic carboxylic acid and A must be Cl or Br, by subjecting to alkynation at the 17α-position the corresponding 17-keto compound if necessary protecting the 3-keto group by ketalization followed by subsequent hydrolysis and a process for the production of a compound of the formula wherein R 1 , R 2 , Z and A are as defined above by subjecting to alkynation in 17α-position a corresponding compound of the formula wherein R 1 and R 2 are as defined above and R is -O alkyl of 1-5 carbon atoms or a cyclic amino radical of the formula wherein n is 4 or 5 and hydrolysing the resultant compound at the 3-position to yield the desired 3-keto compound. Pharmaceutical compositions containing the above compounds of improved anabolic/androgenic ratio which may also possess anti-fertility, anti-androgenic and anti-estrogenic activities may be administered orally or parenterally. |
