Cu-Catalyzed Direct C6-Arylation of Indoles

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• 作者：Youqing Yang ; Ruirui Li ; Yue Zhao ; Dongbing Zhao ; Zhuangzhi Shi
• 刊名：Journal of the American Chemical Society
• 出版年：2016
• 出版时间：July 20, 2016
• 年：2016
• 卷：138
• 期：28
• 页码：8734-8737
• 全文大小：385K
• 年卷期：0
• ISSN：1520-5126

文摘

The first example of direct and site-selective arylation of indoles at the C6 position has been reported. The key to this high regioselectivity is the appropriate choice of the N–P(O)^tBu₂ directing group and the use of diaryliodonium triflate salts as the coupling partners in the presence of catalytic CuO. The protocol is distinguished by mild reaction system that avoids ligand and additives, exhibiting wide scope of indole and arene coupling components without compromising its efficiency and scalability, thus representing a significant advancement in the implementation of regioselective direct arylation of indoles.