One or more nitrogen‐containing molecules constitute an important class of heterocyclic compounds in organic synthesis, due to their reactivity and their presence in many molecules of natural, human or plant origin. These nitrogenous heterocycles play an essential role in various scientific domains, whether they are chemical, biological or pharmacological. N‐heterocycles are the privileged source of many research topics developed by several groups of researchers. Thus, different methods have been developed to access these heterocyclic compounds with nitrogenous rings, such as triazolopyrimidines. In this review, a bibliographic study summarizing the pharmacological importance of the triazolo[1,5‐a]pyrimidine ring, the different synthesis routes of these derivatives as well as their reactivity was reported.

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