王淑静, 沈季铭, 周维善. 抗雌激素△4-10β-乙酰氧基-17β-羟基-17α-乙炔基-雌甾烯-3-酮的合成J. 药学学报, 1982, 17(4): 302-304.
引用本文: 王淑静, 沈季铭, 周维善. 抗雌激素△4-10β-乙酰氧基-17β-羟基-17α-乙炔基-雌甾烯-3-酮的合成J. 药学学报, 1982, 17(4): 302-304.
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WANG Shu-jing, SHEN Ji-ming , CHOU Wei-shan, . SYNTHESIS OF THE ANTI-ESTROGEN, △4-10β-ACETOXY-17β-HYDROXY-17α-ETHYNYLESTREN-3-ONEJ. Acta Pharmaceutica Sinica, 1982, 17(4): 302-304.
Citation: WANG Shu-jing, SHEN Ji-ming , CHOU Wei-shan, . SYNTHESIS OF THE ANTI-ESTROGEN, △4-10β-ACETOXY-17β-HYDROXY-17α-ETHYNYLESTREN-3-ONEJ. Acta Pharmaceutica Sinica, 1982, 17(4): 302-304.
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抗雌激素△4-10β-乙酰氧基-17β-羟基-17α-乙炔基-雌甾烯-3-酮的合成

SYNTHESIS OF THE ANTI-ESTROGEN, △4-10β-ACETOXY-17β-HYDROXY-17α-ETHYNYLESTREN-3-ONE

    摘要
  • Abstract: △4-10β-acetoxy-17β-hydroxy-17α-ethynyl-estren-3-one (1a, R=Ac, R'=H) and its diacetate (R=R'=Ac) were prepared fom compounds (2) or (5) by the reaction sequence shown in scheme 1. In experimental animals 1 a (R=Ac, R'=H) is nearly 100% effective in preventing pregnancy. Compound 1 a (R=Ac, R'=H) has been examined in the clinic. Urfortunately, preliminary results do not confirm the contraceptive potential suggested by the animalstudies.

     

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