An improved and practical route for the synthesis of enzalutamide and potential impurities study

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• 作者：Ai-Nan Zhou^a ; ^b ; Bonan Li^a ; ^{pkuthulbn@gmail.com} ; Lejun Ruan^a ; Yeting Wang^a ; Gengli Duan^b ; Jianqi Li^a ; ^{lijianqib@126.com}
• 关键词：Enzalutamide ; New route ; High purity ; Impurity
• 刊名：Chinese Chemical Letters
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：28
• 期：2
• 页码：426-430
• 全文大小：304 K
• 卷排序：28

文摘

An improved and practical synthesis of enzalutamide was accomplished in five steps. Starting from 4-bromo-2-fluoro-benzonic acid, a methyl esterification, Ullmann ligation, methyl esterification, ring closing reaction and final methyl amidation provided the target in 35% total yield with 99.8% purity. Five identified impurities were also synthesized. This efficient and economical procedure avoids the use of highly toxic reagents and multiple recrystallization operations, which is suitable for further industrialization.