The present invention relates to a process for the preparation of estra-1,3,5(10)- trien-3, 15α, 16α, 17β-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-l,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, wherein A is a protecting group, via said silyl enol ether derivative.
本发明涉及一种制备
雌二醇(estetrol)的过程,通过
硅烯醇醚衍
生物17-B-
氧基-3-A-
氧基-雌
三烯-1,3,5(10),16-四
烯制备,其中A是保护基,B是-Si(R2)3。该发明还涉及一种合成3-A-
氧基-雌
三烯-1,3,5(10),15-四
烯-17-
酮的过程,其中A是保护基,通过上述
硅烯醇醚衍
生物实现。