[1,2,4]三唑并[1,5- a ]嘧啶由于其有价值的生物学特性而非常受关注并且是稠合杂环的趋势类别。一些[1,2,4]-三唑并[1,5- a ]嘧啶具有除草活性，1它们还可以作为抗真菌剂，2抗结核药，3和抗菌药4。据报道，含有[1,2,4]三唑并[1,5- a ]-嘧啶部分的多环系统是抗肿瘤药物，5是促肾上腺皮质激素释放因子1受体拮抗剂6或钙通道调节剂； 7它们可用于治疗阿尔茨海默氏病8 9三唑并嘧啶与Pt和Ru的复合物对寄生虫具有很高的活性10，也可用于治疗癌症。11[1,2,4]三唑并[1,5- a的合成方法]]-嘧啶可分为两个主要组：嘧啶部分环合至三唑环和三唑片段环合至嘧啶环。[1,2,4]三唑并[4,3- a ]嘧啶的Dimroth重排也可用于合成[1,2,4]三唑并[1,5- a ]嘧啶。在这篇综述文章中，我们重点介绍了用于创建[1,2,4]三唑并[1,5- a ]嘧啶体系的合成方法。
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Synthesis of [1,2,4]triazolo[1,5- a ]pyrimidine (microreview)
[1,2,4]Triazolo[1,5-a]pyrimidines are very interesting and trend class of fused heterocycles due to their valuable biological properties. Some [1,2,4]-triazolo[1,5-a]pyrimidines possess herbicidal activity,1 also they can act as antifungal,2 antitubercular,3 and antibacterial4 agents. Polycyclic systems containing [1,2,4]triazolo[1,5-a]-pyrimidine moiety are reported as antitumor,5 as corticotropin-releasing factor 1 receptor antagonists6 or calcium channel modulators;7 they can be used for treatment of Alzheimer's disease8 and insomnia.9 Complexes of triazolo-pyrimidines with Pt and Ru are highly active against parasites10 and can also be used in treating cancer.11The synthetic ways for the preparation of [1,2,4]triazolo[1,5-a]-pyrimidines can be divided into two main groups: annulation of pyrimidine moiety to triazole ring and annulation of triazole fragment to pyrimidine ring. The Dimroth rearrangement of [1,2,4]triazolo[4,3-a]pyrimidines can also be used for the synthesis of [1,2,4]triazolo[1,5-a]pyrimidines. In this review article we have focused on synthetic approaches for the creation of [1,2,4]triazolo[1,5-a]pyrimidine system.
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