Efficient Copper-Mediated Radiosynthesis of 6-[18F]Fluoro-L-DOPA ([18F]FDOPA) in a Microreactor

Objectives

The diagnostic radiopharmaceutical 6-[18F]Fluoro-L-DOPA ([18F]FDOPA) is a versatile positron emission tomography (PET) tracer used to image dopaminergic dysfunction in Parkinson’s disease, brain tumors, and neuroendocrine disorders. Despite its broad clinical applications, [18F]FDOPA production remains challenging. The electron-rich aromatic structure has traditionally necessitated electrophilic [18F]F2 labeling, resulting in low molar activity and potentially increasing the risk of pharmacological effects. Copper-mediated radiofluorination of organoboron precursors using nucleophilic [18F]fluoride provides a promising alternative but remains constrained by lengthy preparation time and high precursor consumption. Here, we developed a microscale copper-mediated radiosynthesis of [18F]FDOPA using a chip-based microreactor.

Methods