Copper-Catalyzed One-Pot Functionalization of Styrenes: Application toward Pharmaceutically Relevant Phenylethylamine Triazole Scaffolds

A Cu-catalyzed, one-pot synthesis of 1,2,3-triazolyl phenylethylamine scaffolds is reported. This method utilizes a single copper catalyst to promote aziridination via nitrene addition, ring-opening with azide, and copper-catalyzed azide-alkyne cycloaddition to afford 1,4-disubstituted 1,2,3-triazole phenylethylamine scaffolds. The utility of this process is demonstrated in the synthesis of pharmaceutically relevant cores from simple styrene motifs.