In organic synthesis, C(sp)-H functionalization is a revolutionary method that allows direct alteration of unactivated C-H bonds. It can obviate the need for pre-functionalization and provides access to streamlined and atom economical routes for the synthesis of complex molecules starting from simple starting materials. Many strategies have evolved, such as photoredox catalysis, organocatalysis, non-directed C-H activation, transiently directed C-H activation, and native functionality directed C-H activation. Together these advances have reinforced the importance of C(sp)-H functionalization in synthetic chemistry. C(sp)-H functionalization has direct applications in pharmacology, agrochemicals, and materials science, demonstrating its ability to transform synthetic approaches by creating new retrosynthetic disconnections and boost the efficiency of chemical processes. This review aims to provide an overview of current state of C(sp)-H functionalization, focusing more on recent breakthroughs and associated mechanistic insights.

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http://dx.doi.org/10.1039/d0cs00488jDOI Listing

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