Abstract
Selective functionalization of one specific C(sp3)–H bond in a complex molecule without the assistance of a directing group represents the state of the art in organic synthesis and will be a dynamic topic in future. In the past decade, many excellent methods have been developed to accomplish this goal with transition-metal catalysts and even under metal-free conditions. In this chapter, we summarize the recent achievements in this realm during the past 5 years, including oxidative functionalization of α-C(sp3)–H bonds adjacent to heteroatoms, allylic, benzylic, and unactivated aliphatic C(sp3)–H bonds. The total redox-neutral C(sp3)–H bond functionalization is also briefly introduced.
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