石杉碱甲的合成研究进展  

Progresses in the Total Synthesis of Huperzine A

作　　者：郑书岩[1] 郁春辉[1] 沈征武[1,2] 

机构地区：[1]上海中医药大学中药学院,上海201203 [2]巴塞利亚药业中国有限公司,海门226100

出　　处：《有机化学》2013年第11期2261-2270,共10页Chinese Journal of Organic Chemistry

摘　　要：石杉碱甲是中国独创的治疗老年痴呆症的药物.由于其显著的疗效,长期以来,一直受到人们的关注和研究.目前石杉碱甲在美国已经进入三期临床研究,而在中国也已获批上市并进入四期临床.由于石杉碱甲在千层塔中的含量仅为万分之一左右,且千层塔的生长周期较长,所以石杉碱甲的化学合成将成为获得该药物的一种有效途径.二十多年来,化学合成石杉碱甲从消旋化合成到手性合成,从毫克级放大到几百克级合成都体现了这一领域的长足发展.其合成工艺和路线也在安全性、实用性方面大为改善.系统综述了1989年到2013年间石杉碱甲化学合成的进展,以期为进一步完善石杉碱甲化学合成提供参考.Huperzine A has been widely used for the treatment of alzheimer in China, and has attracted widespread attention. It has been entered into phase 3 investigation in US and phase 4 investigation in China for the treatment of alzheimer and related disease. Due to the trace content in the herb Huperzia serrata, the chemical synthesis of huperzine A becomes the attractive option for drug supply. During the past two decades, significant progresses have been achieved for the stereoselective synthesis of （-）-huperzine A. The total synthesis of hundreds of grams of （-）-huperzine A has been achieved recently. In addition to the efficiency of the synthesis, the safety of the process was also significantly improved. The progresses of the total synthesis of huperzine A made from 1989 to 2013 are comprehensively reviewed in this paper.

关 键 词：石杉碱甲 化学合成 综述 

分 类 号：TQ464[化学工程—制药化工]