Enantioselective Dearomative Arylation of Isoquinolines

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• 作者：Ming Zhang ; Wangsheng Sun ; Gongming Zhu ; Guangjun Bao ; Bangzhi Zhang ; Liang Hong ; Min Li ; Rui Wang
• 刊名：ACS Catalysis
• 出版年：2016
• 出版时间：August 5, 2016
• 年：2016
• 卷：6
• 期：8
• 页码：5290-5294
• 全文大小：469K
• 年卷期：0
• ISSN：2155-5435

文摘

The C1-substituted tetrahydroisoquinolines and 1,2-dihydroisoquinoline constitute an important group and are interesting structural motifs found in many natural products and pharmaceuticals. In this context, a phosphoric-acid-catalyzed enantioselective dearomative arylation of isoquinolines was realized, providing the chiral dihydroisoquinolines with indole substituents at the C1-position in good results (up to >99% yield and 97% ee). The reaction features mild reaction conditions and operational simplicity, which make it an attractive approach to the discovery of biologically interesting α-indolisoquinolines.