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Direct selective palladium catalyzed C–H functionalization has become a highly attractive strategy in organic synthesis and represents a highly desirable goal. Compared with cross-coupling reactions of C–H bonds with aryl or alkyl halides/pseudohalides, the strategy of cross-coupling reactions of C–H bonds with organometallic reagents is of great significance and obvious advantages. This feature article provides a comprehensive summary of recent advances and an intensive analysis on Pd-catalyzed C–H activation and oxidative coupling with various organometallic reagents.

Graphical abstract: Pd-catalyzed oxidative coupling with organometallic reagents via C–H activation

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