Research Progress in the Preparation of ¹⁸F-DOPA

¹⁸F6-fluoro-3,4-dihydroxy-L-phenylalanine (¹⁸F-DOPA) has been known to be a useful radiotracer for neuropsychiatric diseases and brain malignancies, and it is also abundantly used for visualizing neuroendocrine tumors at present. However, its more widespread clinical use was hampered by the lack of a high specific activity, high yielding labeling method. This review mainly summarized new developments in the synthesis of ¹⁸F-DOPA with electrophilic reactions and nucleophilic substitution reactions in recent years. Among these, considerable advances in nucleophilic synthesis had been achieved by developing novel precursors and utilizing chiral phase-transfer catalysts (cPTC) mediated fluorinations allowing for the production of ¹⁸F-DOPA in high specific activity and high radiochemical yield.