摘要/Abstract

杂环芳烃广泛存在于合成药物和天然产物中，具有多种生物活性.其中，烷基化的杂环芳烃在药物化学与医药工业中扮演着重要的角色，也引起了合成化学家的高度重视.C（sp³）—H断裂的策略由于具有优异的原子经济性，在有机合成中被广泛应用于杂环芳烃的自由基烷基化反应，并且在复杂天然产物及药物分子的合成中都有成功的应用.根据产生自由基的前体化合物的不同（包括醚、醇、胺、酯、酰胺和普通烷烃），综述了近10年来C（sp³）—H断裂的新策略在杂环芳烃自由基烷基化反应中的发展，并对相关机理进行了讨论.
关键词: C-H键断裂, 杂环芳烃, 自由基, 烷基化
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


PDF全文下载地址:

点我下载PDF