<p>Regiospecific method for the synthesis of <i>N</i><sup>9</sup>-alkylated 8-azapurines was proposed based on the reconstructive methodology. It was shown that 2,5-diamino-4-alkylaminopyrimidines under the diazotization reaction conditions were converted into the corresponding 2-amino-<i>N</i><sup>9</sup>-alkyl-8-azapurines in high yields. A possibility for the synthesis of analogs of natural nucleosides, 8-azapurines containing hydroxy groups in the pseudoriboside moiety, was demonstrated, including the synthesis of analog of antiviral drug Penciclovir.</p>

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Regiospecific method for the synthesis of N9-alkylated 8-azapurines

  • K. V. Savateev,
  • D. A. Gazizov,
  • P. A. Slepukhin,
  • V. L. Rusinov

摘要

Regiospecific method for the synthesis of N9-alkylated 8-azapurines was proposed based on the reconstructive methodology. It was shown that 2,5-diamino-4-alkylaminopyrimidines under the diazotization reaction conditions were converted into the corresponding 2-amino-N9-alkyl-8-azapurines in high yields. A possibility for the synthesis of analogs of natural nucleosides, 8-azapurines containing hydroxy groups in the pseudoriboside moiety, was demonstrated, including the synthesis of analog of antiviral drug Penciclovir.