Pyrazolo[1,5-a]pyrimidine scaffold is one of the privileged hetrocycles in drug discovery. Its application as a buliding block for developing drug-like candidates has displayed broad range of medicinal properties such as anticancer, CNS agents, anti-infectious, anti-inflammatory, CRF₁ antagonists and radio diagnostics. The structure-activity relationship (SAR) studies have acquired greater attention amid medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is plenty of room for the medicinal chemists to further exploit this privileged scaffold in developing potential drug candidates. The present review briefly outlines relevant synthetic strategies employed for pyrazolo[1,5-a]pyrimidine derivatives. It also extensively reveals significant biological properties along with SAR studies. To the best of our understanding current review is the first attempt made towards the compilation of significant advances made on pyrazolo[1,5-a]pyrimidines reported since 1980s.

吡唑并[1，5- a ]嘧啶支架是药物发现中的优先杂环化合物之一。它作为开发类似药物的候选药物的药物的应用已显示出广泛的医学特性，例如抗癌药，中枢神经系统药物，抗感染，抗炎药，CRF ₁拮抗剂和放射诊断学。结构-活性关系（SAR）研究在药物化学家中引起了越来越多的关注，并且许多先导化合物是针对各种疾病靶标而衍生的。但是，药物化学家还有足够的空间进一步开发这种特权支架，以开发潜在的候选药物。本综述简要概述了吡唑并[1,5- a]嘧啶衍生物。它也与SAR研究一起广泛揭示了重要的生物学特性。据我们所知，本综述是自1980年代以来首次尝试汇编吡唑并[1,5- a ]嘧啶的重要进展。