Synthesis of lamivudine
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    Abstract:

    Abstract:The synthetic method of typical antivius agent of pyrimidine nucleoside lamivudine is reported.(1R)-(-)-Menthyl glyoxylate hydrate was synthesized from L-menthol and glyoxylic acid by a five-step way including esterification,cyclization,chlorination,condensation and reduction. In the synthesis process of MGH, the perfect molar ratio was n(L-menthol):n(glyoxylic acid)=3:1; In the synthesis process of NA, triphosgene replaced dimethyl sulfoxide and the yield was 60.3%. NA was reduced to lamivudine using sodium borohydride- methanol -THF system,which gave the 84.8% yield.The total yield reached 30.9% and the objective product was characterized with MS and IR

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History
  • Received:December 10,2009
  • Revised:February 15,2010
  • Adopted:February 26,2010
  • Online: May 13,2010
  • Published:
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