Fluorine-18 Labeling of Difluoromethyl and Trifluoromethyl Groups via Monoselective C-F Bond Activation.

We report a general method for the labeling of both CF and CF H groups in a broad range of chemical settings (aryl, oxide, sulfide). The method utilizes frustrated Lewis pair mediated selective C-F activation to formally substitute fluorine-19 with fluorine-18 in a two-step defluorination/radiofluorination process, and as such can utilize the target compounds as starting materials. The radiotracer precursors can be isolated as stable salts prior to radiofluorination.