The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17β-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R2)3.
本发明涉及一种通过
硅基烯醚衍
生物 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene 制备
雌甾-1,3,5(10)-
三烯-3,15a,16a,17β-四醇(estetr-01)的工艺,其中 A 为保护基团,B 为 -Si(R2)3。本发明还涉及一种合成 3-A-氧-
雌甾-1,3,5(10),15-四烯-17-酮的工艺,其中 A 是保护基团,通过
硅基烯醚衍
生物 17-B-氧-3-A-氧-
雌甾-1,3,5(10),16-四烯,B 是-Si(R2)3。