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Directed Amination of Non-Acidic Arene C[BOND]H Bonds by a Copper–Silver Catalytic System


  • We thank the Welch Foundation (E-1571), NIGMS (R01GM077635), Camille and Henry Dreyfus Foundation, and Norman Hackerman Advanced Research Program for supporting this research.


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Amine meets arene: A method for direct amination of β-C(sp2)[BOND]H bonds of benzoic acid derivatives and γ-C(sp2)[BOND]H bonds of benzylamine derivatives has been developed. The reaction is catalyzed by Cu(OAc)2 and a Ag2CO3 cocatalyst, and shows high generality and functional-group tolerance, as well as providing a straightforward means for the preparation of ortho-aminobenzoic acid derivatives.