Copper-mediated nucleophilic radiofluorination of [18 F]β-CFT for positron emission tomography imaging of dopamine transporter.

Hung-Man Yu, Ching-Yun Li, Shiu-Wen Liu, Chun-Hung Yang, Yu Chang

Journal of labelled compounds & radiopharmaceuticals 2021 May 30

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18 F]β-CFT is a positron emission tomography (PET) ligand for imaging of dopamine transporter. It was proved to be a sensitive PET marker to detect presynaptic dopaminergic hypofunction in Parkinson's disease. In recent years, copper-mediated 18 F-fluorination of aryl boronic esters has been successful in some molecules containing aromatic groups. In this study, we describe the novel synthetic strategy of [18 F]β-CFT by copper-mediated nucleophilic radiofluorination with pinacol-derived aryl boronic esters upon reaction with [18 F]KF/K222 and Cu (OTf)2 (py)4 . The radiolabeling protocol was optimized with [18 F]fluoride elution method and amount of copper catalyst used. [18 F]β-CFT is obtained from boronic ester precursors in 2.2% to 10.6% non-isolated radiochemical yield (RCY). Purified [18 F]β-CFT with >99% radiochemical purity (RCP) and high molar activity was obtained in validation runs. The radiolabeling procedure is straightforward and can easily be adapted for clinical use. © 2021 John Wiley & Sons, Ltd.

Citation

Hung-Man Yu, Ching-Yun Li, Shiu-Wen Liu, Chun-Hung Yang, Yu Chang. Copper-mediated nucleophilic radiofluorination of [18 F]β-CFT for positron emission tomography imaging of dopamine transporter. Journal of labelled compounds & radiopharmaceuticals. 2021 May 30;64(6):228-236