The conventional etherification uses toxic or hardly degradable alkylating agents. An eco-friendly tandem etherification/aromatization is presented to prepare estrone 3-secondary ethers from easily available dienone 1. Three marketed 3-etherified estrogen drugs were synthesized with the method from commercial available starting material.
Zheng, Dong-Qing,Jing, Yu,Zheng, Bing-Ying,Ye, Yun-Fei,Xu, Sheng,Tian, Wei-Sheng,Ma, Hai-Yan,Ding, Kai
p. 2164 - 2169
(2016/04/09)
17β-Ethynyl-3,17α-estradiol and derivatives thereof
17β-ethynyl-3,17α-estradiol and derivatives thereof are prepared by epimerization of 17-acyl esters of 17α-ethynyl-3,17β-estradiol 3-ethers. 17α-ethynyl-3,17α-estradiol and its derivatives are active as post-coital antifertility agents and inhibit the growth of or reduce the size of the prostate gland and the seminal vesicle.
