Transition Metal‐Catalyzed Formation of N‐Heterocycles via Aryl‐ or Vinyl C–H Bond Amination

Abstract

Abstract The construction of N‐heterocycles remains a fertile area of research because of their ubiquitous occurrence in biologically active small molecules and materials. Their ubiquitous nature has motivated the development of methods to streamline their synthesis. Formation of the C–N bond via transition metal‐functionalization of the aryl or vinyl C–H bond simplifies N‐heterocycle synthesis by minimizing the manipulation of functional groups. Transition metal‐catalyzed C–H bond amination can be accomplished through two strategies: the activation of the N‐atom or activation of the C–H bond. This microreview examines the recent advances in applying these two strategies for the functionalization of sp 2 C–H bonds and is organized by the source of nitrogen atom.