11β-[4-(N,N-二甲胺基)-苯基]-17α-(丙炔-1)-△^(4,9)-雌甾二烯-17β-羟基-3-酮的制造Ⅳ(RU-486)

PREPARATION OF 11β-[4(N.N-DIMETHYLAMINO)-PHYNYL]-17α-(PROR-1-YNYL)-Δ4,9-ESTRADIENE-17β-O1-3-ONE (Ⅰ Ⅴ)(RU-486)

本文报道了11β—取代17α—丙炔基甾体化合物的合成,并详述了丙炔气体制备的一种简便方法。17α—丙炔基的引入是 RU—486具有抗孕酮和抗糖皮质激素活性的重要基团之一。

The synthesis of one 17 α-(prop-1-ynyl)-11β substituted steroid compound is reported and a simple proc- ess of preparing propyne gass is stated in detail. The introduce of 17α-(prop-1-ynyl) group is one of important groups which leads RU-466 having autiprogesterone and antiglucocorticoid activity.