摘要/Abstract

串联[1，n]-氢迁移/环化反应通过分子内氢负离子迁移，能够使杂原子邻位C（sp³）—H键官能化，把C（sp³）—H键直接转化成为C—C，C—N，C—O等键.此方法在构建五元、六元、七元杂环和全碳环中表现出了巨大的潜力，通过该反应可以高效地合成药物分子中的常见骨架.手性胺、手性路易斯酸以及手性布朗斯特酸等催化剂已经成功地应用于这类反应的不对称催化当中.
关键词: C(sp³)-H键官能化, 串联反应, [1,n]-氢迁移/环化反应, 不对称催化, 杂环化合物
The C (sp³)-H adjacent to heteroatoms can be readily functionalized to C-C, C-N, C-O bonds etc. via cascade[1, n]-hydride transfer/cyclization, which shows high potency to construct 5-membered, 6-membered and all carbon rings. This intriguing cascade process can be employed to synthesize common skeletons of significant natural products and pharmaceutical molecules. Chiral amines, Lewis acids and Brønsted acids have been successfully utilized to catalyze the asymmetric cascade reaction.
Key words: C (sp³)-H functionalization, cascade reaction, [1,n]-hydride transfer/cyclization, asymmetric catalysis, heterocyclic compound


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