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Copper-catalyzed cross-dehydrogenative-coupling (CDC) reactions have been developed as one of attractive methodologies in synthetic chemistry. One of the notable features of this type of the transformation is the selective and efficient functionalization of relatively acidic sp3 C–H bonds with a variety of nucleophiles (X–H) to form sp3 C–X bonds. The significant advantage of this protocol is attributed to the excellent catalytic properties of copper catalysts in sp3 C–H bond oxidation. In this chapter, the progress of Cu-catalyzed C–C and C–heteroatom bond formation through CDC reactions is presented.

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