A Modular Synthetic Approach toward N-Aryl-1,3,4-oxadiazol-2(3H)-one Pharmacophores via Chan–Lam Coupling

Abstract Herein, we report a modular and efficient synthesis of N-aryl-1,3,4-oxadiazol-2(3H)-one pharmacophores via Chan–Lam coupling of oxadiazolones with (hetero)arylboronic acids. This novel protocol employs readily accessible starting materials under mild, operationally simple conditions, along with wide substrate scope, rendering it a practical and versatile approach for the construction of diverse pharmaceutically relevant N-aryl-1,3,4-oxadiazol-2(3H)-one derivatives.