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Cu-Catalyzed Direct Amination of Cyclic Amides via C-OH Bond Activation Using DMF

Peng Chen, Kaixiu Luo, Xianglin Yu, Xu Yuan, Xiaoyu Liu, Jun Lin* and Yi Jin*

*School of Chemical Science and Technology, Yunnan University, Kunming 650091, P.R. China, Email:,

P. Chen, K. Luo, X. Yu, X. Yuan, X. Liu, J. Lin, Y. Jin, Org. Lett., 2020, 22, 6547-6551.

DOI: 10.1021/acs.orglett.0c02320

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A copper-catalyzed direct amination of cyclic amides in DMF forms aromatic heterocyclic amines with readily available reagents via a radical mechanism. The coordinating effect of the N1 atom provides assistance to the copper ions for the activation and amination of C-O bonds.

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Key Words

quinazolines, DTBP

ID: J54-Y2020