Recent Advances in C–H Functionalization of 2H-Indazoles

2H-Indazoles are one class of the most important nitrogen-containing heterocyclic compounds. The 2H-indazole motif is widely present in bioactive natural products and drug molecules that exhibiting distinctive bioactivities. Therefore, much attention has been paid to access diversified 2H-indazole derivatives. Among them, the late-stage functionalization of 2H-indazoles via C–H activation is recognized an efficient approach to increase the complexity and diversity of 2H-indazole derivatives. In this review, we summarized recent achievements on the late-stage functionalization of 2H-indazoles, including the C3-functionalization of 2H-indazole through transition-metal-catalyzed C–H activation or radical pathway, the transition-metal-catalyzed ortho C2’–H functionalization of 2H-indazoles and the remote C–H functionalization of the benzene ring in 2H-indazoles.

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