| 摘要 |
1,202,757. 12 - Methyl - estrapolyenes. ROUSSEL-UCLAF. 12 Dec., 1968 [12 Dec., 1967], No. 59263/68. Heading C2U. The invention comprises (a) compounds of Formula I wherein A is H, carboxylic acyl, or alkyl, and B is H or hydrocarbyl, 12 - methyl - 17# - hydroxy -estra - 4,9,11 - trien - 3 - one (III) excepted; and (b) the 3 - C 2-4 alkylene ketals, 3 - oximes and 3 - o - alkyl - oximes of compounds I wherein A is H, of compound III and of 12 - methyl - estra - 4,9,11 - trien - 3,17 - dione. The 17# - acyloxy and 17# - alkoxy compounds of Formula I are prepared from the corresponding 17#-ols. The 17# - hydroxy - 17α - hydrocarbyl compounds of Formula I are prepared from compound III by successively blocking the 3 - oxo group, oxidizing the 17# - hydroxy group, reacting the resulting 17-one with an appropriate organometallic compound, and freeing the 3-oxo group. The aforementioned ketals, oximes and oalkyl - oximes are prepared during this process. Compound III comprises the subject-matter of Specification 1,202,758. The compounds of Formula I, including 12 - methyl - 17# - hydroxy - estra - 4,9,11 - trien - 3-one, are stated to possess anti-androgenic activity and may be made up with suitable carriers into pharmaceutical compositions suitable for oral, parenteral or rectal administration. |
