Cu(I)-Catalyzed Enantioselective Friedel–Crafts Alkylation of Indoles with 2-Aryl-N-sulfonylaziridines as Alkylating Agents

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• 作者：Chen Ge ; Ren-Rong Liu ; Jian-Rong Gao ; Yi-Xia Jia
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：July 1, 2016
• 年：2016
• 卷：18
• 期：13
• 页码：3122-3125
• 全文大小：323K
• 年卷期：0
• ISSN：1523-7052

文摘

A highly enantioselective Friedel–Crafts alkylation of indoles with N-sulfonylaziridines as alkylating agents has been developed by utilizing the complex of Cu(CH₃CN)₄BF₄/(S)-Segphos as a catalyst. A range of optically active tryptamine derivatives are obtained in good to excellent yields and enantioselectivities (up to >99% ee) via a kinetic resolution process.