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

[18F]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 18F‐fluorination of aryl boronic esters has been successful in some molecules containing aromatic groups. In this study, we describe the novel synthetic strategy of [18F]β‐CFT by copper‐mediated nucleophilic radiofluorination with pinacol‐derived aryl boronic esters upon reaction with [18F]KF/K222 and Cu (OTf)2(py)4. The radiolabeling protocol was optimized with [18F]fluoride elution method and amount of copper catalyst used. [18F]β‐CFT is obtained from boronic ester precursors in 2.2% to 10.6% non‐isolated radiochemical yield (RCY). Purified [18F]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. The novel synthetic strategy of [18F]β‐CFT by copper‐mediated nucleophilic radiofluorination with pinacol‐derived aryl boronic esters upon reaction with [18F]KF/K222 and Cu (OTf)2(py)4 is described. The radiolabeling protocol was optimized with [18F]fluoride elution method and the amount of copper catalyst used. Purified [18F]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.