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Divergent Synthesis of Quinolones and Dihydroepindolidiones via Cu(I)-Catalyzed Cyclization of Anilines with Alkynes

Xuefeng Xu, Ruzhong Sun, Sheng Zhang, Xu Zhang* and Wei Yi*

*College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang 473061; Guangzhou Medical University, Guangzhou, Guangdong 511436, China, Email:,

X. Xu, R. Sun, S. Zhang, X. Zhang, W. Yi, Org. Lett., 2018, 20, 1893-1897.

DOI: 10.1021/acs.orglett.8b00436

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An efficient Cu(I)-catalyzed direct cyclization of readily available primary anilines and alkynes provides diverse 4-quinolones. Thiophenols and phenols are also viable substrates for this reaction. Moreover, secondary arylamines can be converted to dihydroepindolidiones.

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Direct Synthesis of 4-Quinolones via Copper-Catalyzed Intermolecular Cyclization of Anilines and Alkynes

X. Xu, X. Zhang, Org. Lett., 2017, 19, 4984-4987.

Key Words


ID: J54-Y2018