Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (12): 2771-2785.DOI: 10.6023/cjoc201605015 Previous Articles     Next Articles



计立a,b, 吴国锋b, 叶伟东b, 陈新志a   

  1. a 浙江大学化学工程与生物工程学院 杭州 310027;
    b 浙江医药股份有限公司研究院 新昌 312500
  • 收稿日期:2016-05-11 修回日期:2016-07-08 发布日期:2016-08-10
  • 通讯作者: 陈新志
  • 基金资助:

    国家自然科学基金(Nos. 21376213,21476194)、教育部高等学校博士学科点专项科研基金(No. 20120101110062)、浙江省博士后科研项目择优(No. BSH1502096)资助项目.

Review of Total Synthesis of Valienamine

Ji Lia,b, Wu Guofengb, Ye Weidongb, Chen Xinzhia   

  1. a College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027;
    b Research & Development Center, Zhejiang Medicine Co., Ltd, Xinchang 312500
  • Received:2016-05-11 Revised:2016-07-08 Published:2016-08-10
  • Supported by:

    Project supported by the National Science Foundation of China (Nos. 21376213, 21476194), the Doctoral Program of Higher Education of China (No. 20120101110062), and the Postdoctoral Advanced Programs of Zhejiang Province (No. BSH1502096).

Valienamine is an α-glucosidase inhibitor belonging to C7N aminocyclitols that was isolated from the microbial degradation of validoxylamine A with Pseudomonas denitrificans. Moreover, valienamine is also an essential core unit in many kinds of pseudo-oligosaccharidic α-D-glucosidase inhibitors such as validamycins and acarbose. Due to the unique structural feature and interesting biological property, since the first isolation in 1972, a great deal of effort has been devoted to the development of various approaches for the efficient synthesis of valienamine. This review summarizes the 23 synthetic approaches towards valienamine reported in the last thirty years.

Key words: valienamine, C7N aminocyclitols, amino-carbasugars, α-glucosidase inhibitors, total synthesis