<p>The present review is devoted to the main methods for the preparation of [1,2,4]triazolo[1,5-<i>a</i>]pyrimidin-7(4<i>H</i>)-ones (a heterocyclic core of the antiviral drug Triazide®) as a promising model for the design of new analogs exhibiting various types of biological activity, in particular, against coronavirus infection. The review covers the main approaches to the synthesis of triazolopyrimidinones developed over the past 20 years, which include the addition of a pyrimidine ring to the triazole one, the addition of a triazole ring to the pyrimidine one, and the construction of a [1,2,4]triazolo[1,5-a]pyrimidine fragment by transformation of other heterocyclic systems.</p>

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Methods for the construction of [1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-ones

  • A. V. Baklykov,
  • M. I. Valieva,
  • E. D. Ladin,
  • D. N. Lyapustin,
  • D. S. Kopchuk,
  • G. V. Zyryanov,
  • V. L. Rusinov

摘要

The present review is devoted to the main methods for the preparation of [1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-ones (a heterocyclic core of the antiviral drug Triazide®) as a promising model for the design of new analogs exhibiting various types of biological activity, in particular, against coronavirus infection. The review covers the main approaches to the synthesis of triazolopyrimidinones developed over the past 20 years, which include the addition of a pyrimidine ring to the triazole one, the addition of a triazole ring to the pyrimidine one, and the construction of a [1,2,4]triazolo[1,5-a]pyrimidine fragment by transformation of other heterocyclic systems.