A method for the synthesis of 3-(tri/difluoromethyl)-1H-1,2,4-triazol-5(4H)-ones via the cyclization of hydrazinecarboxamides with tri/difluoroacetic anhydride was developed.

An efficient protocol for the synthesis of 5‐aryl‐6‐(trifluoromethyl)‐2,3‐dihydropyrazolo[1,2‐a]pyrazol‐1(5H)‐one derivatives through a copper‐catalyzed [3+2]‐cycloaddition of azomethine imines with 3,3,3‐trifluoropropyne (generated in situ from dehydrobromination of 2‐bromo‐3,3,3‐trifluoropropene under base conditions) is developed. The advantages of this transformation are the broad substrate scope and the good functional group compatibility. The subsequent oxidation and nucleophilic substitution/aromatization provide a new approach to 4‐trifluoromethylated pyrazol‐1‐yl propanoic acids.

A double nucleophilic addition−cyclization− elimination cascade is developed, that allows various 2,6diaryl-4-perfluoroalkylpyridines to be synthesized in one step from easily available enamides and perfluorocarboxylic anhydrides. The procedure is also operationally simple and scalable and provides access to the facial construction of 4fluoroalkylpyridines, which are of great interest in medicinal chemistry.

A copper-mediated three-component reaction of o-iodoanilines, anilines, and ethyl trifluoropyruvate is reported. The transformation allows diverse scopes on both o-iodoanilines and anilines delivering various 2-trifluoromethylbenzimidazole products in moderate to good...