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Issue 2, 2020
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Peroxide-mediated site-specific C–H methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones under metal-free conditions

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Abstract

An effective approach to realize the direct methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones with peroxides under metal-free conditions is described. In this protocol, peroxides serve as both the radical initiator and methyl source. Methylated imidazopyridines and quinoxalin-2(1H)-ones were smoothly synthesized in moderate to good yields. A free radical reaction mechanism was proposed to describe the methylation process.

Graphical abstract: Peroxide-mediated site-specific C–H methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones under metal-free conditions

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Article information


Submitted
28 Oct 2019
Accepted
28 Nov 2019
First published
28 Nov 2019

Org. Biomol. Chem., 2020,18, 205-210
Article type
Communication

Peroxide-mediated site-specific C–H methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones under metal-free conditions

S. Jin, H. Yao, S. Lin, X. You, Y. Yang and Z. Yan, Org. Biomol. Chem., 2020, 18, 205
DOI: 10.1039/C9OB02328C

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