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Copper-Catalyzed Electrophilic Amination of Heteroarenes and Arenes by C[BOND]H Zincation


  • We acknowledge financial support from Duke University and fellowships from the Burroughs Wellcome Endowment (S.L.M.) and the Duke University Pharmacological Sciences Training Program (C.E.H.).


Direct amination of heteroarenes and arenes has been achieved in a one-pot C[BOND]H zincation/copper-catalyzed electrophilic amination procedure. This amination method provides an efficient and rapid approach to access a diverse range of heteroaromatic and aromatic amines including those previously inaccessible using C[BOND]H amination methods. The mild reaction conditions and good functional-group compatibility demonstrate its great potential for the synthesis of important and complex amines.