Synthesis of high-molar-activity [F]6-fluoro-L-DOPA suitable for human use via Cu-mediated fluorination of a BPin precursor.

[F]6-fluoro-L-DOPA ([F]FDOPA) is a diagnostic radiopharmaceutical for positron emission tomography (PET) imaging that is used to image Parkinson's disease, brain tumors, and focal hyperinsulinism of infancy. Despite these important applications, [F]FDOPA PET remains underutilized because of synthetic challenges associated with accessing the radiotracer for clinical use; these stem from the need to radiofluorinate a highly electron-rich catechol ring in the presence of an amino acid. To address this longstanding challenge in the PET radiochemistry community, we have developed a one-pot, two-step synthesis of high-molar-activity [F]FDOPA by Cu-mediated fluorination of a pinacol boronate (BPin) precursor.