| 摘要 |
1528796 7α-Hydroxy-cotradiols SCHERING AG 13 Oct 1975 [14 Oct 1974 8 Aug 1975] 41798/75 Heading C2U Novel steroids of the formula (wherein R 1 is H, acyl, optionally substituted alkyl, cycloalkyl or a saturated oxygen-containing heterocyclic group; R 2 and R 3 are each H, acyl or a saturated oxygen-containing heterocyclic group; and R 4 is a C 1-5 aliphatic hydrocarbon group which may be chloro-substituted if it is unsaturated) are prepared from the corresponding 17-ones and suitable reagents containing R 4 . They may also be obtained by microbiological hydroxylation of the corresponding 7-unsubstituted-17#-ols. In the products OH groups may be esterified or etherified and esters and ethers may be hydrolysed. 3,7α - bis - tetrahydropyranyloxy - #<SP>1,3,5(10)</SP>- estratrien-17-one is prepared from the corresponding 3,7-diol and dihydropyran. 3-Cyclopentyloxy - 7α - hydroxy - #<SP>1,3,5(10)</SP>-estratrien - 17- one is prepared from the same starting material and cyclopentyl bromide. The novel steroids possess a strong vaginotropic and a weak uterotropic action and they are suitable for treatment of estrogen deficiency phenomena, particularly for postmenopausal treatment of women. They may be made up into pharmaceutical compositions with suitable carriers. |
