A facile total synthesis of imatinib base and its analogues

…, CL Wang, YJ Bai, N Han, JP Jiao…

Index: Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495

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Citation Number: 52

Abstract

Imatinib and its analogues were successfully synthesized by an improved method in 19.5– 46.2% total yield of six main steps. Pyrimidinyl amine was prepared by the reaction of enaminone and guanidine nitrate without the use of a toxic cyanamide. N-(2-Methyl-5- nitrophenyl)-4-(pyridin-3-yl) pyrimidin-2-amine as a key intermediate for the synthesis of imatinib was prepared by copper-catalyzed N-arylation of heteroarylamine in 82% yield. ...

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