Advances in the Synthesis of Heteroaryl-1,2,5-oxadiazoles: A Personal Account

Abstract The 1,2,5-oxadiazole ring is an important structural motif in the design of next-generation therapeutic agents and various functional materials. Although chemistry of 1,2,5-oxadiazoles has been known for a while, main recent efforts of researchers in this field are focused on the construction of heteroaryl-substituted 1,2,5-oxadiazoles. A combination of several heterocyclic moieties within a molecule usually provides a synergistic effect on functional properties of the resulting hybrids compared to their parent entities. In this Account, we summarize our recent achievements in the development of straightforward and step-economy methods for the synthesis of heteroaryl-1,2,5-oxadiazoles. Mostly, the presented approaches are based on heterocyclization and/or cycloaddition of 1,2,5-oxadiazole-derived precursors. Potential application perspectives of the presented compounds are also emphasized.