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Copper-Mediated C[BOND]H/C[BOND]H Biaryl Coupling of Benzoic Acid Derivatives and 1,3-Azoles


  • This work was partly supported by Grants-in-Aid from MEXT and JSPS (Japan). M.M. acknowledges Kansai Research Foundation for technology promotion.


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Hot couple: A precious-metal-free copper-mediated intermolecular direct biaryl coupling of benzoic acid derivatives and 1,3-azoles has been developed. The key to success is the installation of an amide-based bidentate coordinating group, which is easily removed and transformed into the parent ester groups after the coupling reaction. Kinetic studies indicate that the rate-limiting step is the aromatic C[BOND]H bond cleavage of benzoic acid derivatives.