Chinese Journal of Organic Chemistry >
Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869
Received date: 2014-02-20
Revised date: 2014-03-06
Online 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
Hou Xuehui , Zhang Jingyu , Liu Hongmin . Synthesis of a Multiple Target Receptor Tyrosine Kinase Inhibitors ABT-869[J]. Chinese Journal of Organic Chemistry, 2014 , 34(6) : 1196 -1200 . DOI: 10.6023/cjoc201402025
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