Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (9): 2676-2680.DOI: 10.6023/cjoc201902020 Previous Articles     Next Articles



沈大冬a, 朱金林b, 吴国锋b, 盛力b, 高浩凌b, 王普a   

  1. a 浙江工业大学药学院 杭州 310032;
    b 浙江医药股份有限公司研究院 绍兴 312500
  • 收稿日期:2019-02-20 修回日期:2019-03-25 发布日期:2019-04-19
  • 通讯作者: 沈大冬, 王普;
  • 基金资助:


Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate

Shen Dadonga, Zhu Jinlinb, Wu Guofengb, Sheng Lib, Gao Haolingb, Wang Pua   

  1. a College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032;
    b Research & Development Center, Zhejiang Medicine Co., Ltd., Shaoxing 312500
  • Received:2019-02-20 Revised:2019-03-25 Published:2019-04-19
  • Contact: 10.6023/cjoc201902020;
  • Supported by:

    Project supported by the Significant New Drugs Development (No. 2008ZX09101-048).

Puquitinib mesylate is a novel phosphatidylinositol 3-kinases (PI3K) inhibitor, which has been shown to be effective in the treatment of cancer. A convenient protocol for the synthesis of the compound at kilogram scale is described, using 2,6-dichloropurine as starting material through amino-protection, SN2 reaction with high regioselectivity, Buchwald-Hartwig coupling reaction, amino-deprotection and salt-forming reaction. The process is easy to operate and provides an effective way at kilogram scale produce with 48% yield in total.

Key words: PI3K inhibitor, puquitinib, synthesis