| 摘要 |
1,231,003. 3,5 - Methyleneoxy - 19 - norsteroids. BEECHAM GROUP Ltd. 5 Dec., 1968 [6 Dec., 1967], No. 55412/67. Heading C2U. Novel compounds of formula (wherein X is H, halo or acyloxy ; Y is H 2 , oxo or (H, OH) ; and Z is a substituent group unchanged by treatment with lead tetra-acetate) are prepared from the corresponding 3#- hydroxy-5#-methyl compounds by reaction with lead tetra-acetate, alone or in the presence of iodine, with heating and/or irradiation in an inert organic solvent. Specified products have (H, C 8 H 17 ) and oxo as values of Z. 5 - Methyl - 19 - nor - 5# - cholest - 9 - ene- 3#,6#-diol 6-acetate (III) is prepared from cholesterol benzyl ether (IV) by the sequence: IV # 3# - benzyloxy - 5,6 - epoxycholestane (5α,6α/5#,6# mixture) # 3# - benzyloxy - 5α- cholestane - 5,6# - diol (V) # the 6 - acetate of V # 3# - benzyloxy - 5 - methyl - 19 - nor- 5#-cholest-9-en-6#-ol acetate # III. 6# - Fluoro - 3# - hydroxy - 5 - methyl - 5#- estr-9-en-17-one (VI) is prepared from 3#- hydroxy - 5 - androsten - 17 - one acetate (VII) by the sequence: VII # 5,6-epoxy-3#- hydroxyandrostan-17-one acetate (which was separated into 5α,6α and 5#,6# epoxides) # 6# - fluoro - 3#,5 - dihydroxy - 5α - androstan-17- one 3-acetate # the acetate of VI # VI. Compounds of the above general formula may be made up with carriers into pharmaceutical compositions. Routes of administration and the nature of the pharmacological activity are not specified. |
