Wang Cong-zhan
2009
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Journal
Chinese Journal of Pharmaceuticals
Abstract
The 5-bromo-3-(trifluoromethyl)phenylamine was reacted with 4-methyl-1H-imidazole in presence of cesium carbonate and cuprous iodide to obtain 3-trifluoromethyl-5-(4-methyl-1H-imidazol-1- yl)phenylamine(4). Ethyl 3-amino-4-methyl benzoate(5) was reacted with cyanamide to obtain the guanidine 6, which cyclized with 3-dimethylamino-1-(3-pyridinyl)-2-propylene-1-one to provide ethyl 4-methyl-3-[[4-(3-pyridinyl)- 2-pyrimidinyl]amino]benzoate(8). Compound 8 was subjected to Boc protection, hydrolysis, amidation and then condensation with compound 4 to give 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[N- tert-butoxycarbonyl-[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzamide(10). After deprotection, the antitumor agent nilotinib was obtained with an overall yield of 40% based on compound 5.