This compound is commonly used as an arylating reagent in organic synthesis especially in cross-coupling photochemical and transition-metal-catalyzed reactions.

The purpose of this reagent is to transfer aryl groups efficiently and selectively during the synthesis of complex organic and pharmaceutical molecules.

(4-Methylphenyl)(246-trimethylphenyl)iodonium trifluoromethanesulfonate is a hypervalent iodine diaryliodonium salt composed of p-tolyl and mesityl aromatic groups with triflate as the counterion.