Recent Progress in Radical Alkylation of Heteroarenes Based on C(sp3)-H bond Cleavage Strategy

doi:10.6023/cjoc202004024

Abstract

Heteroarenes are widely found in synthetic drugs and natural products and exhibit various biological activities. Among them, alkylated heteroarenes play a crucial role in the pharmaceutical industry, and have attracted great attention of synthetic chemists. C(sp³)-H bond cleavage strategy was widely used in radical alkylation of heteroarenes in organic synthesis and has been successfully applied in the total synthesis of natural products and pharmaceuticals due to its excellent atom economy. Based on the different precursor compounds (ethers, alcohols, amines, esters, amides and common alkanes), the research progress of radical alkylation of heteroarenes in a decade is summarized, and the related mechanism is also discussed.

Key words: C-H cleavage, heteroarene, radical, alkylation

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Luo Wenkun, Yang Kai, Yin Biaolin. Recent Progress in Radical Alkylation of Heteroarenes Based on C(sp³)-H bond Cleavage Strategy[J]. Chinese Journal of Organic Chemistry, 2020, 40(8): 2290-2307.

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基于C(sp³)—H键断裂策略的杂环芳烃自由基烷基化反应进展

Recent Progress in Radical Alkylation of Heteroarenes Based on C(sp³)-H bond Cleavage Strategy

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基于C(sp3)—H键断裂策略的杂环芳烃自由基烷基化反应进展