Abstract

An efficient benzylic C–H amidation method was developed through copper-catalyzed C(sp3)−H/N–H cross dehydrogenative coupling between toluene derivatives and N-(8-quinolyl)amides. The 8-quinolyl group directed the activation of N–H bond without influence of quinoline C–H bonds or remote C(sp3)−H bonds. The reaction also showed broad substrate scope with good functional group compatibility, producing various functionalized N-benzyl tertiary amides.

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