| 摘要 |
1,268,241. Linear anthrasteroids. SHIONOGI & CO. Ltd. 3 March, 1969 [1 March, 1968], No. 11305/69. Headings C2C and C2U. Novel compounds I (in which X is where the alkyl group has 1-4C, 1-4C alkylenedioxy or oxo; Y<SP>11</SP> is or 1-4C alkylenedithio or benzylthio when the conjugated diene structure is present in the C ring; D is H or halo; a wavy line represents a or # configuration; and a broken line represents an optional further bond) and when the compounds are acylable, their esters including cyclic esters are prepared by general methods as illustrated in the following sequences in which Ac is an acyl group. Steroid intermediates isolated are 3α, 20#- diacetyloxy - 8α,9α- dihydroxy - 5α- pregnan - 11- 11 - one; 8α,9α- dihydroxy - 5α- androstanone; 3# - acetyloxy - 11 - oxo - 5α- androstane- 8α,9α- diol; 17# - acetyloxy - 11 - oxo - 5α- androstane - 8α,9α- diol, 3#,17# - diacetyloxy- 11 - oxo - 5α- androstane - 8α,9α- diol and 20# - acetyloxy - 11 - oxo - pregnane - 8α,9α- diol all prepared by reaction of the appropriate 8(9)- ene with ruthenium or osmium tetroxide. Other intermediates isolated are the 8,9,11- trioxo - 8,9 - seco - steroids corresponding to the above steroid intermediates prepared by reaction of said steroid intermediates with lead tetraacetate or a periodate. Pharmaceutical compositions comprise a compound I together with a suitable pharmaceutical diluent or carrier and are administered orally or parenterally as anti-androgenic agents; diuretics; and anti-fertility, anti-inflammatory, anti-pituitary and anti-lipemic agents. |
