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在甾体分子的9-位、11-位引入二个双键往往可以增强或改变其生理活性,例如18-甲基三烯炔诺酮与三烯炔诺酮均有比母体18-甲基炔诺酮与炔诺酮更强的抗生育活性。将11-位双键改为11-位酮基,即在11-位引入氧原子,则有抗着床与降胆固醇作用,11-酮基-△~9-炔诺酮(9)100ν对大鼠有抗着床作用,法国Roussel-Uclaf公司进行了全合成,并作简单报道。我们采用炔诺酮中间体,19-羟基-△~4-雄甾烯-3,17-二酮(1)为原料,用半合成路线仅8步反应合成了化合物(9)。
The introduction of two double bonds at the 9-position and 11-position of a steroid molecule often enhances or alters its physiological activity. For example, both 18-methyltrostanoic acid and norethindrone are more active than the parent 18-methyl Norethisterone and norethindrone stronger anti-fertility activity. By changing the 11-position double bond to the 11-position keto group, that is introducing anti-implantation and cholesterol lowering effect by introducing oxygen atom at 11-position, Rat anti-implantation effect, the French company Roussel-Uclaf fully synthesized and made a simple report. Using norethindrone intermediate and 19-hydroxy-Δ4-androstene-3,17-dione (1) as raw materials, we synthesized compound (9) in only 8 steps by semi-synthetic route.