| 摘要 |
1341601 4,14-Estradienes ALTON OCHSNER MEDICAL FOUNDATION 27 April 1971 [28 April 1970 5 Feb 1971] 11602/71 Heading C2U The invention comprises compounds of formula wherein R is H or Me and R<SP>1</SP> is H or COR<SP>11</SP>, where R<SP>11</SP> is C 1-10 alkyl, C 6-15 aryl (optionally substituted by one or more C 1-7 alkyl groups), C 3-8 cycloalkyl or C 7-15 aralkyl (optionally substituted on the aryl ring by one or more C 1-7 alkyl groups). Compound I (R = R<SP>1</SP> H) is prepared from estrone 3-methyl ether (II) by the sequence: II -# 16α - bromo - II -# 14 - dehydro - II (+15 - dehydro - 14 - epi - II by-product) -# 14 - dehydroestradiol 3 - methyl ether -# 3- methoxyestra - 2,5(10),14 - trien - 17# - ol -# the #<SP>5(10)</SP>-isomer of I -# I. The penultimate product may not be isolated. Compound I (R=Me, R<SP>1</SP>=H) is prepared analogously. Compounds I (R<SP>1</SP> = COR<SP>11</SP>) are prepared by conventional esterification of I (R<SP>1</SP> = H). Compounds I are said to possess anabolic and androgenic activity, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration. |
