HFIP-Promoted [18F] trifluoromethylation via iodofluorination of gem-difluoroalkenes

Abstract

Herein, we report a novel hydrogen-bond-assisted radiofluorination strategy for the trifluoromethylation of gem-difluoroalkenes, utilizing NIS as the activator and HFIP as the essential solvent to facilitate key hydrogen-bonding interactions. This method demonstrates broad functional group compatibility, delivers high radiochemical yields, and provides an efficient route to α-iodo-[¹⁸F]trifluoromethylated alkanes. These features position the protocol as a valuable tool for the rapid construction of novel positron emission tomography (PET) tracers.