Nucleophilic Synthesis of 6-l-[(18)F]FDOPA. Is Copper-Mediated Radiofluorination the Answer?

Positron emission tomography employing 6-l-[(18)F]fluoro-3,4-dihydroxyphenylalanine (6-l-[(18)F]FDOPA) is currently a highly relevant clinical tool for detection of gliomas, neuroendocrine tumors and evaluation of Parkinson’s disease progression. Yet, the deficiencies of electrophilic synthesis of 6-l-[(18)F]FDOPA hold back its wider use. To fulfill growing clinical demands for this radiotracer, novel synthetic strategies via direct nucleophilic (18)F-radiloabeling starting from multi-Curie amounts of [(18)F]fluoride, have been recently introduced. In particular, Cu-mediated radiofluorination of arylpinacol boronates and arylstannanes show significant promise for introduction into clinical practice. In this short review these current developments will be discussed with a focus on their applicability to automation.