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Regioselective Synthesis of Acylated N-Heterocycles via the Cascade Reactions of Saturated Cyclic Amines with 2-Oxo-2-arylacetic Acids

Xiaonan Shi, Xi Chen, Muhua Wang, Xinying Zhang* and Xuesen Fan*

*School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China, Email:,

X. Shi, X. Chen, M. Wang, X. Zhang, X. Fan, J. Org. Chem., 2018, 83, 6524-6533.

DOI: 10.1021/acs.joc.8b00805

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Cascade reactions of saturated cyclic amines with 2-oxo-2-arylacetic acids enable a highly regioselective and versatile synthesis of acylated N-heterocycles. In this cascade process, the copper catalyst is believed to play a crucial role not only in dehydrogenation but also in the decarboxylation and cross coupling reaction.

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Key Words

1,2,3,4-tetrahydropyridines, 2-pyrrolines, DTBP

ID: J42-Y2018