朱莉亚, 林紫云, 韩广甸. 3,5-甾二烯化合物的合成及抗早孕活性J. 药学学报, 1993, 28(5): 347-351.
引用本文: 朱莉亚, 林紫云, 韩广甸. 3,5-甾二烯化合物的合成及抗早孕活性J. 药学学报, 1993, 28(5): 347-351.
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LY Zhu, ZY Lin , GD Han, . SYNTHESIS OF GONA-3,5-DIENES AND STUDIES ON THEIR ACTIVITY FOR INTERRUPTION OF EARLY PREGNANCYJ. Acta Pharmaceutica Sinica, 1993, 28(5): 347-351.
Citation: LY Zhu, ZY Lin , GD Han, . SYNTHESIS OF GONA-3,5-DIENES AND STUDIES ON THEIR ACTIVITY FOR INTERRUPTION OF EARLY PREGNANCYJ. Acta Pharmaceutica Sinica, 1993, 28(5): 347-351.
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3,5-甾二烯化合物的合成及抗早孕活性

SYNTHESIS OF GONA-3,5-DIENES AND STUDIES ON THEIR ACTIVITY FOR INTERRUPTION OF EARLY PREGNANCY

    摘要
  • 摘要: 以18-甲基-17β-羟基-17α-乙炔基-雌甾-4-烯-3-酮(18-甲基炔诺酮),17β-羟基-17α-乙缺基-雌甾-4-烯-3-酮(炔诺酮),17β-羟基-17α-乙炔基-雄甾-4-烯-3-酮(妊娠素)和17a-羟基孕甾-4-烯-3,20二酮(17α-羟基黄体酮)为原料,经NaBH,还原、脱水、双键转位和酯化等反应合成一系列3,5-甾二烯化合物,用1HNMR和MS证明了它们的结构。动物筛选结果表明,17β-丙酰氧基-17α-乙炔基-雌甾-3,5-二烯(IVb2有明显的抗早孕活性。中断早期妊娠的作用似与其雌激素活性有关。

     

    Abstract: A series of gona-3,5-dienes were synthesized from norgestrel, norethisterone 17α-hydroxyprogesterone and ethisterone via reduction of α,β-unsaturated 3-ketones to allylic alcohols and dehydration with concomitant migration of the double bond. The structures of these gona-3,5-dienes were verified by MS and 1H-NMR spectral data.Pharmacological results showed that compound IVb2 in this series gave rise to significant interruption of early pregnancy in mice. The mechanism of the early pregnancy terminating effect of this compound was discussed.

     

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