有机化学 ›› 2011, Vol. 31 ›› Issue (10): 1563-1572. 上一篇    下一篇

综述与进展

一类α-五元杂环氨基酸的合成研究进展

孙晓敏1,张伟2,丁宁2,王鹏1,李英霞*,2   

  1. (1中国海洋大学医药学院 教育部海洋药物重点实验室 青岛 266003)
    (2复旦大学药学院 上海 201203)
  • 收稿日期:2011-01-05 修回日期:2011-03-13 发布日期:2011-03-21
  • 通讯作者: 李英霞 E-mail:liyx417@fudan.edu.cn

Progress in the Synthesis of One Kind of α-Heterocycle Five-Membered Amino Acids

Sun Xiaomin1 Zhang Wei2 Ding Ning2 Wang Peng1 Li Yingxia*,2   

  1. (1 School of Pharmacy, Ocean University of China, Qingdao 266003)
    (2 School of Pharmacy, Fudan University, Shanghai 201203)
  • Received:2011-01-05 Revised:2011-03-13 Published:2011-03-21

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.

关键词: α-五元杂环氨基酸, 环化脱水, 生物合成, 仿生合成

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.

Key words: α-heterocycle five-membered amino acids, cyclodehydration, biosynthesis, biomimetic synthesis