| 摘要 |
PURPOSE:To obtain a new steroid derivative efficiently and stereoselectively synthesizable by synthetic organic chemical technique without the need for using natural substance-derived materials with problems such as concerning resource security, having proliferation inhibitory activity against oncocytes, thus useful as an antineoplastic agent etc. CONSTITUTION:This new steroid derivative having antineoplastic activity is expressed by formula I (R is a 1-13C alkyl; A is hydroxyl group or a group becoming hydroxyl group through ready hydrolysis; X and Y are combined into oxo or a 2-3C alkylenedioxy; X is hydroxyl, a 1-5C alkoxyl or a group becoming hydroxyl group through ready hydrolysis; Y is H or 1-5C alkoxyl; when X is hydroxyl or a group becoming hydroxyl through ready hydrolysis, Y is H; when X is a 1-5C alkoxyl, Y is also a 1-5C alkoxyl). This new compound can be obtained by protecting the hydroxyl group of 3beta,12beta-dihydroxy-5alpha- pregnan-20-one followed by alkylation with a Grignard reagent and dehydration and then Oppenauer oxidation of the product which is, in turn, treated with a peroxide. |
