Novel method for manufacturing of N-(5-[4-[4-methyl-piperazino-methyl]benzolamido)-2-methylphenyl-4-[3-pyridyl]-2-pyrimidin-amine
The present invention refers to dif luoro antitumor Ν-5-[ 4-(4-methyl-piperazino-methyl)-benzoyl amido]-4-methyl phenyl-2-(3-pyridyl)-2-pyrimidine-amine novel manufacturing method relates to, the present invention according to manufacturing method flat plate is transferred to print the shortened response time product of high purity and in high yields and a merchandise after looking at it in, efficient, economic and method is a more environmentally friendly while.
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Paragraph 0111; 0112
(2016/12/12)
A facile total synthesis of imatinib base and its analogues
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 coppercatalyzed iV-arylation of heteroarylamme in 82% yield. The copper salts were used instead of the expensive palladium compounds in this C-N bond-forming reaction. The intermediate nitro compound was reduced by a N2H 4.H2O/FeCl3/C system using water as a solvent in good yield.