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Copper-Catalyzed Oxalamide-Directed ortho-C–H Amination of Anilines with Alkylamines

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journal contribution
posted on 2020-06-16, 18:34 authored by Peng Wu, Wei Huang, Tai-Jin Cheng, Hai-Xia Lin, Hui Xu, Hui-Xiong Dai
A copper-catalyzed oxalamide-directed ortho-C–H amination of anilines has been developed by using 1 atm of air as the sole oxidant. The protocol shows excellent functional group tolerance, and some heterocyclic amines including indole, benzothiophene, benzothiazole, quinoline, isoquinoline, and quinoxaline could be compatible in the reaction. The late-stage diversification of medicinal drugs demonstrates the synthetic utility of this protocol.