An Overview on Synthetic and Medicinal Perspectives of [1,2,4]Triazolo[1,5‐a]pyrimidine Scaffold

Abstract [1,2,4]Triazolo[1,5‐ a ]pyrimidine is an important heterocyclic scaffold known to have a wide range of pharmacological activities such as anticancer, antimicrobial, anti‐tubercular, CB 2 cannabinoid agonists, feticide, and adenosine antagonists. Several clinical trials and marketed drugs such as Trapidil, Essramycin, Pyroxsulam, DSM‐265, Flumetsulam, GNF‐6702, and Cevipabulin indicate the potential of [1,2,4]triazolo[1,5‐ a ]pyrimidine moiety with various functional groups in medicinal chemistry. Herein, we represent a concise report focusing on the synthetic strategies used for diversely substituted [1,2,4]triazolo[1,5‐ a ]pyrimidine analogs and their pharmacological applications. To the best of our knowledge, since 1980, we are the first to write a review on this emerging scaffold, which reveals the synthetic strategies, and pharmacological activities of differently substituted [1,2,4]triazolo[1,5‐ a ]pyrimidine with special emphasis on structure‐activity relationship studies.