摘要/Abstract

苯丙氨酸衍生物具有显著的生物活性，被广泛应用于药物分子中.主要综述了近年来基于苯丙氨酸衍生物的碳氢键直接官能化反应，有效构建了C—I，C—C[含C（sp²）—C（sp²），C（sp²）—C（sp）和C（sp²）—C（sp³）键]，C—N，C—B和C—O键，从而简洁、高效地实现了苯丙氨酸衍生物的邻位碘化及分子内胺化反应，邻位烷基化、芳基化、烯基化、炔基化、酰基化、酰氧基化、胺化和硼化反应，以及间位芳基化和烷基化反应等.
关键词: 苯丙氨酸, C-H键官能化, 烷基化, 烯基化, 芳基化
Phenylalanine derivatives are widely found in a broad range of pharmaceutical molecules and exhibit significant biological activity. Direct C-H bond functionalization of phenylalanine derivatives to offer an efficient approach to construct C-I, C(sp²)-C(sp²), C(sp²)-C(sp), C(sp²)-C(sp³), C-N, C-B and C-O bonds is described. The transformation involves ortho-C-H bond iodination and the following intramolecular amination, ortho-alkylation, ortho-arylation, ortho-alkenylation, ortho-alkynylation, ortho-acylation, ortho-acetoxylation, ortho-amination, ortho-boronation, meta-arylation and meta-alky-lation.
Key words: phenylalanine, C-H functionalization, alkylation, alkenylation, arylation


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