Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate

doi:10.6023/cjoc201902020

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

NOTE

磷脂酰基醇3-激酶抑制剂甲磺酸普喹替尼的合成

沈大冬^a, 朱金林^b, 吴国锋^b, 盛力^b, 高浩凌^b, 王普^a

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 E-mail:shendadong@126.com;wangpu@zjut.edu.cn
基金资助:
重大新药创制（No.2008ZX09101-048）资助项目.

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

Received:2019-02-20 Revised:2019-03-25 Published:2019-04-19
Contact: 10.6023/cjoc201902020 E-mail:shendadong@126.com;wangpu@zjut.edu.cn
Supported by:
Project supported by the Significant New Drugs Development (No. 2008ZX09101-048).

1. Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate.PDF(1365KB)

Abstract

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.

Key words: PI3K inhibitor, puquitinib, synthesis

Cite this article

Shen Dadong, Zhu Jinlin, Wu Guofeng, Sheng Li, Gao Haoling, Wang Pu. Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate[J]. Chin. J. Org. Chem., 2019, 39(9): 2676-2680.

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磷脂酰基醇3-激酶抑制剂甲磺酸普喹替尼的合成

Development of Synthesis of Phosphatidylinositol 3-Kinases Inhibitor Puquitinib Mesylate

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