Automatic Production of [¹⁸F]F-DOPA Using the Raytest SynChrom R&D Module

Area of Science:

• Radiochemistry
• Nuclear Medicine
• PET Imaging

Background:

• [18F]F-DOPA is a crucial positron emission tomography (PET) tracer for diagnosing various conditions including Parkinson's disease, gliomas, and neuroendocrine tumors.
• Previous radiosynthesis methods for [18F]F-DOPA suffered from low efficiency and purity, limiting clinical utility.
• Despite being known for over 30 years, advancements in synthesis are needed for widespread clinical adoption.

Purpose of the Study:

• To develop and optimize a robust radiosynthesis method for producing high-purity [18F]F-DOPA suitable for clinical PET diagnostics.
• To evaluate the efficiency and purity of the synthesized [18F]F-DOPA using a specific automated synthesis module.

Main Methods:

• Fluorine-18 ([18F]) labeling was achieved via nucleophilic substitution using the ABX 1336 precursor.
• The synthesis involved anion exchange, elution, fluorination, intermediate purification (C18ec column), Baeyer-Villiger oxidation, hydrolysis, and final purification (semi-preparative column).
• Radiosynthesis was performed on a Raytest Synchrom R&D module, with reactions monitored and optimized.

Main Results:

• The optimized radiosynthesis successfully produced [18F]F-DOPA within 120 minutes.
• Achieved a radiochemical yield (RCY) of 15%.
• Demonstrated high radiochemical purity (RCP) of ≥ 97% and enantiomeric purity (ee) of ≥ 96%.

Conclusions:

• The developed nucleophilic radiosynthesis method provides a reliable and efficient route to high-quality [18F]F-DOPA.
• The achieved yield and purity meet the stringent requirements for clinical PET imaging applications.
• This optimized synthesis facilitates the broader diagnostic use of [18F]F-DOPA in neurology and oncology.