Direct Synthesis of 4-Quinolones via Copper-Catalyzed Intermolecular Cyclization of Anilines and Alkynes
Xuefeng Xu and Xu Zhang*
*College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang 473061, China, Email: zhangxuedu126.com
X. Xu, X. Zhang, Org. Lett., 2017, 19, 4984-4987.
DOI: 10.1021/acs.orglett.7b02495 (free Supporting Information)
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A Cu-catalyzed formation of 4-quinolones from simple and readily available anilines and alkynes offers mild reaction conditions, high functional-group tolerance, and amenability to gram-scale synthesis. Under optimized conditions, both N-alkyl- and N-aryl-substituted anilines can be successfully transformed into the corresponding 4-quinolones.
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X. Xu, R. Sun, S. Zhang, X. Zhang, W. Yi, Org. Lett., 2018, 20, 1893-1897.