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7α和7β-甲基-10β,17β-二乙酰氧基-4-雌甾烯-3-酮的合成
引用本文:倪元,郝日英,周维善.7α和7β-甲基-10β,17β-二乙酰氧基-4-雌甾烯-3-酮的合成[J].药学学报,1987,22(7):495-500.
作者姓名:倪元  郝日英  周维善
作者单位:中国科学院上海有机化学研究所
摘    要:由于7α-甲基或10β-乙酰氧基4(5)烯-3-酮雌(雄)甾化合物具有显著的抗着床或抗蜕膜活性,我们合成了既具有7α-甲基或7β-甲基又具有10β-乙酰氧基的两个新甾族化合物(1a)和(1b)。经药理试验表明(1a)和(1b)对孕鼠均有抗早孕作用。

关 键 词:7α-甲基-10β  17β-二乙酰氧基-4-雌甾烯-3-酮  7β-甲基-10β  17β-二乙酰氧基-4-雌甾烯-3-酮  抗生育
收稿时间:1986-05-19

Synthesis of 7 alpha-methyl and 7 beta-methyl-10 beta, 17 beta-diacetoxy-4-estrene-3-one
NI Yuan,HAO Ri-Ying and ZHOU Wei-Shan.Synthesis of 7 alpha-methyl and 7 beta-methyl-10 beta, 17 beta-diacetoxy-4-estrene-3-one[J].Acta Pharmaceutica Sinica,1987,22(7):495-500.
Authors:NI Yuan  HAO Ri-Ying and ZHOU Wei-Shan
Abstract:Since 7α-methyl or 10β-acetoxyestrene-3-ketones were known to show significant anti-implantational or anti-decidual activities, we have synthesized two new steroidal ketones (1a). and (1b) possessing both the 7α-or 7β-methyl group and the 10β-acetoxy substitutions according to scheme 1.Experimental animal tests of (1a) showed that it was effective for termination of early pregnancy on mice with the success rate of 100% (4mg/kg). (1a) is approximately 3~4 times more potent than (1b). Results of parmacological tests have been reported elsewhere.
Keywords:7β-Methyl-10β  17β-diacetoxy-4-estrene-3-one  Antifertility  7α-Methyl-10β  17β-diacetoxy-4-estrene-3-one
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