A novel synthetic process of flecainide acetate
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Guangzhou Baihua Flavours And Fragrgances Co.,Ltd.

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TQ463

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    Abstract:

    flecainide acetate was synthesized from methyl 5-bromo-2-iodobenzoic acid via Ullmann aryl etherification, amide condensation, salification. The total yield was 52.1% (based on methyl 5-bromo-2-iodobenzoic acid). The optimistic condition of Ullmann aryl etherification reaction was established. The reaction conditions were obtained as follows: when{[(phen)2Cu][OCH2CF3]Cu} is used as ligand. The reaction was stirred in DMF at 110℃for 12 hours. The yield of key intermediate is 60.1%. The total yield of flecainide acetateis 54.0%, and the purity is 99.93%. The structure of flecainide acetate and the important intermediates were confirmed by MS, 1H NMR.

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History
  • Received:August 24,2022
  • Revised:December 09,2022
  • Adopted:December 09,2022
  • Online: April 13,2023
  • Published: September 30,2022
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