有机化学 ›› 2013, Vol. 33 ›› Issue (06): 1144-1156.DOI: 10.6023/cjoc201304035 上一篇    下一篇

综述与进展

3,4-桥环吲哚类生物碱的合成研究进展

单冬, 贾彦兴   

  1. 北京大学药学院 天然药物及仿生药物国家重点实验室 北京 100191
  • 收稿日期:2013-04-22 修回日期:2013-05-13 发布日期:2013-05-15
  • 通讯作者: 贾彦兴 E-mail:yxjia@bjmu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21290180, 20972007);国家重点基础研究发展规划(973计划, No.2010CB833200)和国家教育部博士点基金(No.20120001110100)资助项目.

Progress in Synthesis of 3,4-Fused Indole Alkaloids

Shan Dong, Jia Yanxing   

  1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191
  • Received:2013-04-22 Revised:2013-05-13 Published:2013-05-15
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.21290180, 20972007), the National Basic Research Program of China (973 Program) (No.2010CB833200) and the Ph.D.Programs Foundation of Ministry of Education of China (No.20120001110100).

取代的吲哚类天然产物是自然界中普遍存在的一类杂环化合物, 由于其具有广泛的生理活性, 以及相当一部分作为重要的临床使用药物, 100多年以来, 吲哚的合成及官能团化一直是有机合成化学家关注的一个重要领域.在众多吲哚类生物碱中, 含有3,4-桥环吲哚骨架的天然产物占据了相当一部分, 由于其独特的结构和良好的生物活性, 这些分子引起了有机合成化学家的广泛兴趣.重点概述了构建3,4-桥环骨架的主要合成方法和策略, 并对一些方法在天然产物全合成中的应用作简要介绍.

关键词: 吲哚生物碱, 3,4-桥环吲哚, 天然产物, 全合成

The indole nucleus is one of the most important heterocycles for its presence in a vast number of bioactive natural products, pharmaceuticals, and agrochemicals.Due to their widest spectrum of biological activity and some of them have been used in clinical trials, construction and functionalization of indoles have attracted considerable interests from synthetic and medicinal chemists for over a hundred years.Among the naturally occurring indole alkaloids, those containing 3,4-fused indole skeleton possess a major part and have been especially considered attractive synthetic targets because of their unique structure and biological activities.This review emphasized on the methodologies and strategies of construction of 3,4-fused indole skeleton, and their application in total synthesis of natural products.

Key words: indole alkaloids, 3,4-fused indoles, natural products, total synthesis