Radiodifluoromethylation of well-functionalized molecules.

Abstract

The strategic installation of a [¹⁸F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [¹⁸F]CF₂H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [¹⁸F]difluorocarbene building block and frustrated Lewis pair-mediated C-¹⁸F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF₂H-containing molecules for drug discovery and PET ligand development.