Recent advances in C-H functionalization of 2 H-indazoles

Org Biomol Chem. 2022 Oct 12;20(39):7746-7764. doi: 10.1039/d2ob01463g.

Abstract

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 exhibit distinctive bioactivities. Therefore, much attention has been paid to access diverse 2H-indazole derivatives. Among them, the late-stage functionalization of 2H-indazoles via C-H activation is recognized as an efficient approach for increasing the complexity and diversity of 2H-indazole derivatives. In this review, we summarized recent achievements in the late-stage functionalization of 2H-indazoles, including the C3-functionalization of 2H-indazoles through transition metal-catalyzed C-H activation or a radical pathway, transition metal-catalyzed ortho C2'-H functionalization of 2H-indazoles and remote C-H functionalization at the benzene ring in 2H-indazoles.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzene
  • Biological Products*
  • Heterocyclic Compounds*
  • Indazoles / pharmacology
  • Nitrogen

Substances

  • Biological Products
  • Heterocyclic Compounds
  • Indazoles
  • Benzene
  • Nitrogen