杂环位于氨基酸C-末端羧基与α-碳之间的α-五元杂环氨基酸是一类主要来源于海洋多肽的高度修饰的氨基酸,分子中杂环的存在对化合物的生物活性有着重要的影响.综述了此类氨基酸的合成方法,这些方法针对不同的底物在操作简便性、收率、产物光学纯度、适用范围上有着明显差别.
Amino acids containing five-membered heterocycles coming between the terminal carbonyl of the acid function and the α-carbon are a class of highly modified amino acids mainly from marine peptides.The five-membered heterocycles are pharmacophores of many natural and synthetic bioactive compounds.This review focuses on the progress of the synthetic methods of these amino acids(including the limitation,simplicity,yield and optical purity) in recent years.