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

Abstract

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.