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


侯学会a, 张京玉b, 刘宏民c   

  1. 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;
  • 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 Xuehuia, Zhang Jingyub, Liu Hongminc   

  1. 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