抗癌天然产物苦马豆素的合成研究进展ProgressintheSynthesisof.PDF

2009 年第 29 卷 有 机 化 学 Vol. 29, 2009 第 5 期, 689～695 Chinese Journal of Organic Chemistry No. 5, 689～695 ·综述与进展· 抗癌天然产物苦马豆素的合成研究进展 叶思杰 刘建利* 黄伟平 (西北大学生命科学院 西部资源生物与现代生物技术省部共建教育部重点实验室 西安 710069) 摘要 在过去十多年中, 多羟基吲哚兹定生物碱因其结构和多样性的生物活性(抗病毒、抗肿瘤、免疫调节活性)而引起 了极大的关注. 其中最著名的成员是苦马豆素, 一种从灰苦马豆等植物中提取出来的化合物, 被证明具有治疗恶性肿 瘤的作用并因此进行了大量合成研究. 到目前为止文献报道的合成方法都是基于碳水化合物原料或非碳水化合物底物 和不对称反应. 尽管有些合成路线有效并且有实用价值, 但进一步开发制备天然或非天然吲哚兹定生物碱的通用和实 用方法仍然非常重要. 总结了苦马毒素的合成研究进展, 以便为它的规模化生产提供思路和方法. 关键词 苦马豆素; 合成; 抗癌 Progress in the Synthesis of Anticancer Natural Product Swainsonine Ye, Sijie Liu, Jianli* Huang, Weiping (Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, School of Life Science, Northwest University, Xian 710069) Abstract Over the past decade, polyhydroxylated indolizidine alkaloids have received considerable atten- tion because of their interesting structures and their diverse biological activities (e.g., antiviral, antitumor, and immunomodulating activities). The most well-known member swainsonine, a natural product isolated from Swainsona canescens, is a potential chemotherapeutic agent for the treatment of cancer and accord- ingly has attracted much synthetic effort. Numerous syntheses documented to date are based on carbohydrate starting materials or asymmetric reactions using non-carbohydrate substrates. Although some syntheses are efficient and useful, further development of general and practical methods for the preparation of natural and unnatural polyhydroxylated