加兰他敏全合成研究进展ProgressesinTotalSynthesisofGalantamine.PDFVIP

2011 年第 31 卷 有 机 化 学 Vol. 31, 2011 第 3 期, 286～296 Chinese Journal of Organic Chemistry No. 3, 286～296 ·综述与进展· 加兰他敏全合成研究进展 房 雷 a,b 苟少华*,a,b 张奕华 c (a 东南大学化学化工学院药物研究中心 南京 210009) (b 江苏省生物药物高技术研究重点实验室 连云 222000) (c 中国药科大学新药研究中心 南京 210009) 摘要 加兰他敏为天然生物碱, 具有乙酰胆碱酯酶抑制及神经元烟碱受体构象调节双重活性, 临床应用非常广泛. 迄 今, 研究人员已提出多种合成策略, 如分子内酚氧化缩合法、分子内 Heck 反应法等, 重点关注近几年加兰他敏全合成 的研究进展, 并尝试对现有方法的发展演变以及各自特点进行综述. 关键词 加兰他敏; 全合成; 研究进展 Progresses in Total Synthesis of Galantamine Fang, Leia,b Gou, Shaohua*,a,b Zhang, Yihuac a ( Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 210009) (b Jiangsu Province Hi-Tech Key Laboratory for Bio-medical Research , Lianyungang 222000) (c Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009) Abstract Galantamine, a natural alkaloid possessing AChE inhibitory and neuronal nicotinic receptor al- losteric modulating effect, is widely used in clinic. Up to date, several different synthetic strategies have been developed for the total synthesis of galantamine, including the phenolic oxidative coupling reaction, the intramolecular Heck reaction, and so on. In this review, the recent progresses in the total synthesis of galan- tamine are reviewed. Furthermore, the evolution and the features of the existing strategies are also discussed. Keywords galantamine; total