Copper( i )-catalyzed azide–alkyne cycloaddition (CuAAC) provides an efficient synthesis of 1,4-disubstituted 1,2,3-triazoles. This feature article highlights the recent progress on the regisoselective synthesis of multisubstituted 1,2,3-triazoles, which current click reaction (CuAAC) is unable to do.

The introduction of trifluoromethyl groups into organic molecules has attracted great attention in the past five years. In this review, we describe the recent efforts in the development of trifluoromethylation via copper catalysis using nucleophilic, electrophilic or radical trifluoromethylation reagents.