Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (11): 2818-2840.DOI: 10.6023/cjoc201705022 Previous Articles     Next Articles



聂飚a, 金传飞a, 钟文和a, 任青云a,b, 张英俊a,b, 张霁a,b   

  1. a 广东东阳光集团药业研究院 东莞 523871;
    b 抗感染新药研发国家重点实验室 东莞 523871
  • 收稿日期:2017-05-16 修回日期:2017-06-20 发布日期:2017-07-14
  • 通讯作者: 张霁
  • 基金资助:


Application and Recent Progress of Phosphoramidate Prodrugs Strategies and ProTide Technology in Drug Discovery

Nie Biaoa, Jin Chuanfeia, Zhong Wenhea, Ren Qingyuna,b, Zhang Yingjuna,b, Zhang Jia,b   

  1. a State Key Laboratory of Anti-infective Drug Development, Dongguan 523871;
    b HEC Pharm Group, HEC R&D Center, Dongguan 523871
  • Received:2017-05-16 Revised:2017-06-20 Published:2017-07-14
  • Contact: 10.6023/cjoc201705022
  • Supported by:

    Project supported by the Introduction of Innovative R&D Team Program of Guangdong Province (No. 201301Y0105381261) and the State Key Laboratory of Anti-Infective Drug Development (Sunshine Lake Pharma Co. Ltd) (No. 2015DQ780357).

This review provides the brief history for the development and advances of ProTide strategies in the field of antiviral and anticancer pharmaceutical development. A summary is provided for the synthesis of nucleoside phosphoramidates, recent breakthroughs in the stereoselective assembly of chiral prodrugs and its application. This technology is extremely useful and has simplified innovative drug design of phosphorous-containing prodrugs. Simplifying such structural modification may create a new avenue of competition in the invention of new medicines from the parent drug.

Key words: phosphoramidates:prodrugs, nucleoside and nucleotide, antiviral drug, phosphate and phosphonate, ProTide