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

△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.     

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

根据文献报道△~4-10β,17β-双羟基-17α-乙炔基-雌甾烯-3-酮(1a,R=H)具有抗雌激素的活性。抗雌激素的药物一般具有抗生育的作用。又据文献报道在具有19-去甲基-结构的甾体避孕药中某些位置羟基的酯化往往增加生理活性或变为口服有效或兼而有之。所以我们合成了10β-乙酰氧基衍生物(1b,R=COCH_3)。合成10β-乙酰氧基甾体     

猪胆汁中胆烷酸的分离和鉴定

猪胆汁皂化提取之猪脱氧胆酸(1a)的重结晶母液,经甲酯化、柱层析分离可得到猪脱氧胆酸甲酯(1b,7.5%)、鹅脱氧胆酸甲酯(2b,61.8%)、猪胆酸甲酯(3b,2.5%)、3α-羟基-6-氧代-5α-胆烷酸甲酯(4b,3.5%)和微量的3α-羟基-6-氧代-5β-胆烷酸甲酯(5b)。