3,4-桥环吲哚类生物碱的合成研究进展有机化学.pdfVIP

DOI: 10.6023/cjoc201304035 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 3,4-桥环吲哚类生物碱的合成研究进展 单 冬 贾彦兴* (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) 摘要 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 Progress in Synthesis of 3,4-Fused Indole Alkaloids Shan, Dong Jia, Yanxing* (State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191) Abstract 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 in- dole 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