Weiguo Wang, Jingyu Wang, Chunpeng Qiu, Kaiyue Dou, Xu Li, Younan Wang
ABSTRACT An efficient strategy for the modular synthesis of fully substituted 5‐thioureido‐triazoles via a transition‐metal‐free KO t Bu‐catalyzed three‐component reaction has been developed. The reaction proceeded through the cycloaddition of nitriles and azides in the presence of a base, followed by the capture of triazolamine and triazole nitrogen anion intermediate with isothiocyanates. This transformation not only features in being transition‐metal‐free and mild reaction conditions, but also displays broad functional group tolerance. The practicality of this method has been demonstrated by further synthetic transformations and late‐stage functionalization of bioactive molecules.