Zang Jia-liang, Chen Yi-fen, Jie Yafei
2009
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0
Influential Citations
1
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Journal
Chinese Journal of Pharmaceuticals
Abstract
2-Chloro-6-methylaniline was acetylated with(E)-3-ethoxyacryloyl chloride to give(E)-N-(2- chloro-6-methylphenyl) -3-ethoxyacrylamide,from which the key intermediate 2-amino-N-(2-chloro-6-methylphenyl)-5- thiazolecarboxamide(5) was obtained by one-pot reaction with N-bromosuccinimide and H_2O,and then thiourea. The chloro groups of 4,6-dichloro-2-methylpyrimidine were successively substituted with amino group of 5,and N-hydroxyethylpiperazine to give antitumor agent dasatinib monohydrate in 52%overall yield.