A facile total synthesis of imatinib base and its analogues

  • Liu Y
  • Wang C
  • Bai Y
 et al. 
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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- catalyzedN-arylation of heteroarylamine in82%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 N2H4 ·H2O/FeCl3/C system using water as a solvent in good yield.

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  • Yi Feng Liu

  • Cui Ling Wang

  • Ya Jun Bai

  • Ning Han

  • Jun Ping Jiao

  • Xiao Li Qi

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