Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869

doi:10.6023/cjoc201402025

Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (6): 1196-1200.DOI: 10.6023/cjoc201402025 Previous Articles Next Articles

多靶点受体酪氨酸激酶抑制剂ABT-869的有效合成方法

侯学会^a, 张京玉^b, 刘宏民^c

a. 河南牧业经济学院质量检测与管理系郑州 450011;
b. 河南中医学院药学院郑州 450008;
c. 郑州大学药学院郑州 450001

收稿日期:2014-02-20 修回日期:2014-03-06 发布日期:2014-03-13
通讯作者: 侯学会, 刘宏民 E-mail:jyzhang2004@126.com;liuhm@zzu.edu.cn
基金资助:
河南省教育厅科学技术研究重点（Nos. 14A150052，12A150026）、郑州市科技攻关计划（No. 121PPTGG509-2）资助项目.

Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869

Hou Xuehui^a, Zhang Jingyu^b, Liu Hongmin^c

a. Department of Quality Detection and Management, Henan University of Animal Husbandry and Economy, Zhengzhou 450011;
b. Henan University of Traditional Chinese Medicine, Zhengzhou 450008;
c. School of Pharmaceutical Science, Zhengzhou University, Zhengzhou 450001

Received:2014-02-20 Revised:2014-03-06 Published:2014-03-13
Supported by:
Project supported by the Education Department of Henan Province Science and Technology Research Projects (Nos. 14A150052, 12A150026), the Scientific Research Plan of Zhenzhou (No. 121PPTGG509-2).

An efficient and convenient protocol for the synthesis of ABT-869, which is a multiple target receptor tyrosine kinase inhibitors with novel structure and high inhibitory activity, was developed in seven steps from cheap and commercially available of 3-fluoroaniline. The target molecular was obtained in 42.3% overall yield without any traditional purification (column chromatography or crystallization). Ultrasonic reaction technology was introduced in the Suzuki coupling reaction which is the key step of the preparation of ABT-869. The synthetic process was more suitable for industrialized production due to the advantages of available starting material, simplicity and cheapness, well yield and purity (HPLC>99.0%).

Key words: receptor tyrosine kinase inhibitors, ABT-869, synthesis

Cite this article

Hou Xuehui, Zhang Jingyu, Liu Hongmin. Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869[J]. Chin. J. Org. Chem., 2014, 34(6): 1196-1200.

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多靶点受体酪氨酸激酶抑制剂ABT-869的有效合成方法

Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869

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