Synthesis of 5-fluoro-6-ethyl-4- hydroxy-pyrimidine
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TQ460.31

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    Abstract:

    The key intermediate of voriconazole, 5-fluoro-6-ethyl-4-hydroxy-pyrimidine was synthesized by a "One pot" ammoniated and cyclization reaction with α-fluoro-ethyl propionyl as raw material. The optimal reaction conditions is: sodium methoxid, ammonia stirred in methanol at room temperature for 5 hours, then added carboxamide; stirred under reflux for another 5 hours; the over all yield of is 63%.

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History
  • Received:December 18,2012
  • Revised:January 23,2013
  • Adopted:January 30,2013
  • Online: May 03,2013
  • Published: