Nucleophilic Synthesis of 6-<span style="font-variant: small-caps">l</span>-[¹⁸F]FDOPA. Is Copper-Mediated Radiofluorination the Answer?

Abstract

Positron emission tomography employing 6-l-[18F]fluoro-3,4-dihydroxyphenylalanine (6-l-[18F]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-[18F]FDOPA hold back its wider use. To fulfill growing clinical demands for this radiotracer, novel synthetic strategies via direct nucleophilic 18F-radiloabeling starting from multi-Curie amounts of [18F]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.

Keywords

• ¹⁸F
• l-[¹⁸F]FDOPA%22%2C%22default_operator%22%3A%22AND%22%7D%7D%7D"> 6-<span style="font-variant: small-caps">l</span>-[¹⁸F]FDOPA
• nucleophilic radiolabeling
• copper-mediated
• organoborons
• organostannanes