化学
多巴胺转运体
亲核细胞
正电子发射断层摄影术
芳基
硼酸
吡那考
多巴胺质膜转运蛋白
放射化学
铜
核化学
组合化学
运输机
核医学
催化作用
有机化学
生物化学
医学
烷基
基因
作者
Hung-Man Yu,Ching-Yun Li,Shiu-Wen Liu,Cheng Yang,Yu Chang
摘要
[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.
科研通智能强力驱动
Strongly Powered by AbleSci AI