a series of 5,6-seco-6,6-dimethyl-6-silasteroids. X-ray crystallographic analysis of 17 and the 17α-ethynyl derivative of 15 confirmed the stereochemical assignments. None of the compounds which were subjected to uterotropic, anti-uterotropic, or post-coital assays, showed significant activity. A partially completed synthesis of 6-silaestradiol (21a) is described.
通过改进的文献方法制备4,4-二甲基-6-甲氧基-4-sila-1-四氢
萘酮(2)并转化为3-甲氧基-6,6-二甲基-6-silaestra-1,3,5( 10),8,14-
戊烯-17β-
乙酸乙烯酯(5c)。5c的催化加氢得到3-甲氧基-6,6-二甲基-6-silaestra-1,3,5(10),8-四烯-17β-
乙酸乙烯酯(6b)及其14-异-和Δ1 , 3,5(10),8(14)异构体,其比例随催化剂和溶剂的不同而变化。用
锂-液
氨还原6b,并进行O-去甲基化,得到6,6-二甲基-6-
硅雌二醇(8b)。
锂-液
氨-t还原8b的3-甲基醚-
丁醇和
水解得到3-keto-6,6-dimethyl-6-silaestr-1(10)-en-17β-ol(15),它被催化还原成1,1α-dihydro衍
生物17。8b,15及其衍
生物的5,6SiC键被
三溴化硼水溶液裂解。
乙醇氟化氢和其他试剂,提供一系列5