Improved Synthesis of Dabigatran Etexilate
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R973 .2

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    Abstract:

    The dabigatran etexilate(Ⅳ) was synthesized from Ethyl 3-(2-(((4-cyanophenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate by Pinner reaction and Acylation Reaction. The structure was confirmed by IR, 1H NMR and ESI-MS. The influencing factors of intermediate Ⅱ, Ⅲ and target compound dabigatran etexilate (Ⅳ) in the synthetic reactions were investigated. The optimized overall yield was 53.6%, which was superior to literature.

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History
  • Received:October 31,2014
  • Revised:December 13,2014
  • Adopted:December 25,2014
  • Online: February 09,2015
  • Published:
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