| 摘要 |
1450439 19-Oxygenated steroids RICHARDSON-MERRELL Inc 20 Dec 1973 [5 Feb 1973] 59128/73 Heading C2U The invention comprises compounds of formula where R 2 is CO or CH(#-OR 5 ); R 3 is H, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; R 1 , R 4 and R 5 are each H, C 1-3 alkyl, C 1-12 acyl, tri- (C 1-5 alkyl)silyl, triphenylsilyl, 2-tetrahydropyranyl, C 5-7 1-cycloalkenyl, or 1-(C 1-2 alkoxy)-C 5-7 cycloalkyl; or R 3 and OR 4 together represent oxo; with the provisos that (i) when R 1 is H or acyl then R 4 cannot be H, acyl or 2-tetrahydropyranyl and R 3 + OR 4 cannot be oxo, and (ii) when R 1 is 2-tetrahydropyranyl and R 2 is CO then R 3 + OR 4 cannot be oxo. Preparation is from 19-hydroxyandrost-4-ene- 3,17-dione, 17#,19-dihydroxy-17α-R 3 -androst- 4-en-3-one or 3#,17#,19-trihydroxyandrost-4- ene by one or more conventional conversions at positions 3,17 and 19 selected from etherification, esterification, ester cleavage, carbonyl reduction, and pyrolysis of 1<SP>1</SP>-alkoxycycloalkoxy to 1<SP>1</SP>-cycloalkenyloxy. "Libido-enhancing" oral and parenteral compositions comprise a compound I and a carrier. |
