Nucleophilic 18F-Fluorination of Anilines via N-Arylsydnone Intermediates

Preparation of [F-18]fluoroarenes with nucleophilic [F-18]fluoride for positron emission tomography (PET) molecular imaging research is a challenging chemical endeavor. Advances in radiofluorination have soared in the last decade, broadening the availability of potential [F-18]fluoroarenes. In this Synpacts article, we highlight the recent development from our laboratory of a practical radiofluorination of anilines via N-arylsydnone intermediates to afford [F-18]fluoroarenes. Further, we emphasize the utility of this methodology towards peptide labeling applications by preparing an F-18-labeled neuropeptide. 1 Introduction 2 Nucleophilic Radiofluorination of N-Arylsydnones 3 Substrate Scope and Applications 4 Conclusion