Copper‐catalyzed C(sp3)−H/N−H Cross Dehydrogenative Coupling Between Toluene Derivatives and Picolinamides

Abstract An efficient C−N bond formation method through copper‐catalyzed C(sp3)−H/N−H cross dehydrogenative coupling between toluene derivatives and picolinamides was developed. The N−H bond of picolinamides was activated by the direction of pyridyl group without influence of remote C−H bonds. The method was applicable to a broad range of substrates with good functional group compatibility, which provided a novel route to prepare N‐benzyl tertiary amides from cheap and readily available starting materials.