A novel Cu-catalyzed direct amidation of 2-methylquinolines with amines is described. This method afforded an efficient approach for the synthesis of biologically important aromatic amides from readily available coupling partners using molecular oxygen as the oxidant.

Copper-catalyzed direct amidation of 2-methylquinolines with amines efficiently synthesizes biologically important aromatic amides using readily available coupling partners and molecular oxygen as an oxidant.

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Copper-catalyzed efficient direct amidation of 2-methylquinolines with amines.

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