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Base-Promoted β-C(sp3)-H Functionalization of Enaminones: An Approach to Polysubstituted Pyridines

Jinhai Shen, Dingding Cai, Changsheng Kuai, Yunqi Liu, Ming'e Wei, Guolin Cheng and Xiuling Cui*

*Institutes of Molecular Medicine and School of Biomedical Sciences, Huaqiao University & Engineering Research Center of Molecular Medicine, Ministry of Education, Xiamen 361021, China, Email:

J. Shen, D. Cai, C. Kuai, Y. Liu, M. Wei, G. Cheng, X. Cui, J. Org. Chem., 2015, 80, 6584-6589.

DOI: 10.1021/acs.joc.5b00635

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A convenient base-promoted reaction of 1-arylethylamines with ynones gives polysubstituted pyridines via direct β-C(sp3)-H functionalization of enaminones under metal-free conditions. This procedure features high regioselectivity, high efficiency, and environmental friendliness. Various polysubstituted pyridines were provided in high yields.

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Key Words

pyridines, oxygen

ID: J42-Y2015