Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (2): 337-361.DOI: 10.6023/cjoc201408007 Previous Articles     Next Articles



张霁, 聂飚, 张英俊   

  1. 广东东阳光集团药业研究院 东莞 523871
  • 收稿日期:2014-08-06 修回日期:2014-09-24 发布日期:2014-11-03
  • 通讯作者: 张霁
  • 基金资助:

    广东省引进创新创业团队计划(No. 201301Y0105381261)资助项目.

Application and Progress of Organic Synthesis in the Discovery of Innovative Drugs

Zhang Ji, Nie Biao, Zhang Yingjun   

  1. HEC Pharm Group, HEC R&D Center, Dongguan 523871
  • Received:2014-08-06 Revised:2014-09-24 Published:2014-11-03
  • Supported by:

    Project supported by the Guangdong Innovative and Entrepreneurial Research Team Program (No. 201301Y0105381261).

This article reviews the application and progress of modern synthetic methods to deliver several innovative drugs, especially the blockbusters, such as sofosbuvir, rivaroxaban, enzalutamide, canagliflozin and tofacitinib. Some of the modern synthetic methods, for example catalytic processes, application of ring-closing metathesis, palladium catalyzed cross-coupling, green chemistry and telescoping of processes, are highlighted. The exciting journey from discovering these new molecular entities, especially those which are first-in-class with the synthesis of a dozen of approved drugs, is described as case studies to fully illustrate the important role of modern organic synthesis for successful drug discovery and development.

Key words: drugs, drug synthesis, organic synthesis, art in drug synthesis