A Practical Preparation of Imatinib Base

作者：Zhang, Xu; Sun, Jingjing; Chen, Tian; Yang, Chenggen; Yu, Lei^*

来源：Synlett, 2016, 27(15): 2233-2236.

DOI：10.1055/s-0035-1562498

• practical method
• total synthesis
• medicinal chemistry
• imatinib
• copper

A practical preparation of imatinib base was reported in this article. Compared with reported works, the features of this work were the concise procedures, the industrially available starting materials, the avoidance of expensive or highly toxic transition-metal catalysts or reagents, and the genotoxic impurities 6-methyl-N-1-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine and 4-(chloromethyl)-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide. The method was scalable to at least 100 mmol, and the products were separated by simple recrystallizations.

• 出版日期2016-9
• 单位扬州大学