Citation: Shen Dadong, Zhu Jinlin, Wu Guofeng, Sheng Li, Gao Haoling, Wang Pu. Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate[J]. Chinese Journal of Organic Chemistry, ;2019, 39(9): 2676-2680. doi: 10.6023/cjoc201902020 shu

Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate

Shen Dadong ^a,, ,
Zhu Jinlin ^b ,
Wu Guofeng ^b ,
Sheng Li ^b ,
Gao Haoling ^b ,
Wang Pu ^a,,

a.
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032
b.
Research & Development Center, Zhejiang Medicine Co., Ltd., Shaoxing 312500

Corresponding author: Shen Dadong, shendadong@126.com Wang Pu, wangpu@zjut.edu.cn
Received Date: 20 February 2019
Revised Date: 25 March 2019
Available Online: 19 September 2019
Fund Project: the Significant New Drugs Development 2008ZX09101-048Project supported by the Significant New Drugs Development (No. 2008ZX09101-048)

Figures(4)

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, S_N2 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.
- PI3K inhibitor,
- puquitinib,
- synthesis
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