噁拉戈利的合成研究进展  

Recent Progress in the Synthesis of Elagolix

作　　者：曾凯强 薛晓文[2] 李嘉宾 ZENG Kaiqiang;XUE Xiaowen;LI Jiabin(College of Sciences,China Pharmaceutical University,Nanjing 211198;College of Pharmaceutical Sciences,China Pharmaceutical Universiy,Nanjing 211989)

机构地区：[1]中国药科大学理学院,江苏南京211198 [2]中国药科大学药学院,江苏南京211198

出　　处：《中国医药工业杂志》2021年第3期320-329,共10页Chinese Journal of Pharmaceuticals

摘　　要：噁拉戈利是一种促性腺激素释放激素拮抗药,2018年FDA通过优先评审批准上市,临床上用于子宫内膜异位症的治疗。本文从逆合成分析入手,梳理了5条噁拉戈利的合成路线,并从反应步数、总收率、原料试剂成本、工艺条件及安全性等方面对各路线进行了比较和分析,最后介绍了氘代噁拉戈利的合成方法,为该类药物及其氘代物的合成工艺研究提供有益参考。Elagolix was a gonadotropin-releasing hormone antagonist.It was approved in 2018 by FDA via priority review for clinical treatment of endometriosis.Based on retrosynthetic analysis,five reported synthesis routes of elagolix were summarized.They were compared and evaluated in terms of step numbers,total yields,costs,synthetic conditions and manufacturing safety.At last,the synthetic method of d_(6)-elagolix was introduced.This review would be beneficial to the future process researches of elagolix and its deuterium analogues.

关 键 词：噁拉戈利 促性腺激素释放激素 拮抗药 子宫内膜异位症 合成 氘代药物 

分 类 号：R914.5[医药卫生—药物化学]