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DOI: 10.1055/s-0036-1588073
Recent Developments in the Direct Methylation of Electron-Deficient N-Heteroarenes
Publication History
Received: 24 August 2016
Accepted after revision: 29 August 2016
Publication Date:
05 September 2016 (online)
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Abstract
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
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For selected examples of metal-catalyzed C–H alkylation of electron-deficient N-heteroarenes, see:
For selected examples of radical-mediated C–H alkylation of electron-deficient N-heteroarenes, see:
For selected examples of transition-metal-free C–H alkylation of electron-deficient N-heteroarenes, see: