Recent Advances in the Transition-Metal-Free Arylation of Hetero­arenes

Transition-metal-free arylation reactions have attracted considerable attention for economic and environmental reasons over the past 40 years. In recent years, much effort has been made to develop efficient transition-metal-free approaches for the arylation of heteroarenes. Covering the literature from 2015 to early 2021, this review aims to provide a thorough overview of the synthetic and mechanistic aspects of these atom-economical and environmentally benign reactions.

1 Introduction

2 Arylation of Pre-functionalized Heteroarenes

2.1 Arylation of Heteroaryl Halides

2.2 Decarboxylative Arylation of Heteroarenes

3 Direct C–H Arylation of Heteroarenes

3.1 C(sp2)–H Arylation

3.2 C(sp3)–H Arylation

4 N-Arylation of Heteroarenes

5 Summary and Outlook