The article highlights the challenges and opportunities in the development of the piperazine-fused triazoles. Approaches toward medicinal chemistry relevant building blocks based on [1,2,4]triazolo[4,3-a]pyrazine platform were elaborated. The methods provide quick and multigram access to the target derivatives starting from commercially available nonexpensive reagents. The approaches were used to create a small library of the triazolopyrazines with variety of substituents in position 3. The potential of further synthetic application of the library members for medicinally oriented synthesis was shown.

中文翻译：

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5,6,7,8-四氢[1,2,4]三唑并[4,3-a]吡嗪的聚焦小分子库：药物化学之家的一块砖

本文重点介绍了哌嗪稠合三唑类药物发展中的挑战和机遇。阐述了基于[1,2,4]三唑并[4,3- a ]吡嗪平台的药物化学相关构建模块的方法。该方法可以从市售的廉价试剂开始快速、多克地获得目标衍生物。这些方法用于创建一个小型的三唑并吡嗪文库，其中 3 位具有多种取代基。显示了文库成员进一步合成应用用于药物合成的潜力。