Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (11): 2261-2270.DOI: 10.6023/cjoc201306006 Previous Articles     Next Articles



郑书岩a, 郁春辉a, 沈征武a,b   

  1. a 上海中医药大学中药学院 上海 201203;
    b 巴塞利亚药业中国有限公司 海门 226100
  • 收稿日期:2013-06-05 修回日期:2013-07-18 出版日期:2013-11-25 发布日期:2013-07-26
  • 通讯作者: 沈征武

Progresses in the Total Synthesis of Huperzine A

Zheng Shuyana, Yu Chunhuia, Shen Zhengwua,b   

  1. a School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203;
    b Basilea Pharmaceutical China Ltd., Haimen 226100
  • Received:2013-06-05 Revised:2013-07-18 Online:2013-11-25 Published:2013-07-26

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.

Key words: huperzine A, chemical synthesis, review