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邻-羟基雌甾化合物是雌甾类物质在体内的主要代谢产物,具有特异的生理活性而女性化作用又减失,对其合成方法与生理活性的研究近年来一直受到广泛的注意。1960年,Fishman等用多步反应合成2-和4-羟基雌酚酮。1973年,Gelbke等用氧化-还原反应合成2-和4-羟基雌甾化合物,产率较低,所用氧化剂[NO(SO_3K)_2]制备困难,性质不稳定,能自发分解爆炸。1974年,专利报道苯甲酰氧自由基法合成2-羟基雌酚酮,可惜此法既未见直接用于2-羟基炔雌醇的类似合成,又难于得到
O-hydroxyestradiol is the main metabolite of estrogen in the body, with specific physiological activity and feminization loss, and the research on its synthesis and physiological activity has been widely paid attention in recent years. In 1960, Fishman et al. Used multistep reactions to synthesize 2- and 4-hydroxystrone. In 1973, Gelbke et al. Used oxidation-reduction reactions to synthesize 2- and 4-hydroxysteroid compounds with low yields. The oxidant [NO (SO 3 K) 2] used was difficult to prepare and was unstable in nature and spontaneously exploded. In 1974, the patent reports benzoyl oxygen free radical synthesis of 2-hydroxy-estrone, but this method is neither directly used for similar synthesis of 2-hydroxy-ethinylestradiol, and difficult to obtain