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醋酸乌利司他关键中间体的合成工艺

杨旭, 候美娇,张翔,董敏,董金华

Chinese Journal of Synthetic Chemistry（2021）

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Abstract
3,20-二(亚乙二氧基)-17α-羟基-19-去甲孕甾-5(10),9(11)-二烯为合成选择性孕酮受体调节剂醋酸乌利司他(Ulipristal Acetate)的关键中间体.以环-3-(1,2-亚乙基缩醛)-雌甾-5(10),9(11)-二烯-3,17-二酮(UPA-O)为原料,经亲核取代、亲核加成、Mislow-Evans重排、醚键断裂、烯醇式互变、缩酮保护等反应,制备该关键中间体.对合成路线中反应条件进行工艺优化,总收率74.8％.
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