Synlett 2016; 27(18): 2525-2529
DOI: 10.1055/s-0036-1588073
© Georg Thieme Verlag Stuttgart · New York

Recent Developments in the Direct Methylation of Electron-­Deficient N-Heteroarenes

Junghoon Kim, Seung Hwan Cho*
  • Department of Chemistry and Division of Advanced Nuclear Engineering, Pohang University of Science and Technology (POSTECH), Pohang, 790-784, Republic of Korea   Email:
Further Information

Publication History

Received: 24 August 2016

Accepted after revision: 29 August 2016

Publication Date:
05 September 2016 (eFirst)


The direct introduction of methyl groups into electron-deficient N-heteroarenes has recently emerged as an efficient and promising strategy to afford methylated N-heteroarenes, which are important motifs in a variety of pharmaceuticals and biologically active molecules. Herein, three general state-of-the-art approaches including radical-mediated, transition-metal-catalyzed, or transition-metal-free direct C–H methylations of electron-deficient N-heteroarenes are highlighted.

1 Introduction

2 Radical-Mediated Methylation of Electron-Deficient N-Heteroarenes

3 Transition-Metal-Catalyzed Methylation of Electron-Deficient N-Heteroarenes

4 Transition-Metal-Free Methylation of Electron-Deficient N-Heteroarenes

5 Conclusions