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This review is focused on the recent advances in the transition metal-catalyzed direct remote C–H-functionalization of alkyl groups via C(sp3)–H bond activation. In general, carboxamide/ester-chelated β-functionalization reactions are summarized, which mainly include direct β-arylation, β-alkylation, β-alkynylation, etc. Additionally, some biologically interesting architectures are constructed by using these direct β-functionalization reactions.

Graphical abstract: Transition metal-catalyzed direct remote C–H functionalization of alkyl groups via C(sp3)–H bond activation

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