Trifluoromethanesulfinyl chloride: an effective trifluoromethyl radical source in the trifluoromethylimination of alkenes

Abstract

The trifluoromethyl (CF₃) group has emerged as a privileged structural motif in pharmaceutical compounds and biologically active molecules, leading to a significant demand for efficient synthetic methodologies to incorporate the trifluoromethyl moiety. In this study, we reported an efficient method with trifluoromethanesulfinyl chloride as a versatile CF₃ source to achieve catalyst-free, highly regioselective intermolecular trifluoromethylimination of alkenes. This practical approach enables efficient access to valuable β-trifluoromethylamine derivatives, offering promising opportunities for structural diversification in drug discovery applications.