| 摘要 |
1,198,847. B-Homosteroids. SANDOZ Ltd. 12 July, 1967 [21 July, 1966; 20 Dec., 1966; 13 April, 1967], No. 32159/67. Heading C2C. The invention comprises compounds of the formula wherein Y is C 1-4 alkyl; R<SP>1</SP> is C 1-3 -#-alkyl; R<SP>5</SP> is #-OH or C 2-20 -#-alkanoyloxy and R<SP>6</SP> isα-H, or R<SP>5</SP> and R<SP>6</SP> together signify oxo. The 17-oxo compounds are prepared by acid cyclization of the corresponding 8,14-seco-B-homogona-1,3,5- (10), 8-tetraen-14,17-diones, or 8,14-seco-B- homogona - 1,3,5(10),9(11) - tetraen - 14,17- diones. The 17-hydroxy compounds are prepared by complex hydride reduction of the corresponding 17-ones. The 17-alkanoyloxy compounds are prepared by acid cyclization of the corresponding 8,14-seco-B-homogona-1,3,5- (10),9(11)-tetraen-14-ones, or by alkanoylation of the corresponding 17-ols. 17# - Acetoxy - 3 - methozy - 13 - methyl - 8,14- seco - B - homogona- 1,3,5(10),9(11) - tetraen - 14- one is prepared from the corresponding 17#-ol, which in turn is prepared from the corresponding 14,17-dione by the action of Saccharomyces uvarum. Compounds of Formula (I) are said to be indicated in the treatment of female hypogonadism, amenorrhea, functional uterine bleeding, osteoporosis and menopausal problems, and for achieving ovulation block, lipid shifting and blood cholesteral-lowering, and may be made up with carriers or diluents into pharmaceutical compositions for oral or parenteral administration.
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