Improved preparation and chemical kinetics on fully automated synthesis of [¹⁸F]-THK523, a PET imaging probe for Tau pathologies

分类： 核科学技术 >> 核材料与工艺技术 提交时间： 2023-06-18 合作期刊: 《Nuclear Science and Techniques》

KONG Yan-Yan SI Zhan CAO Guo-Xian ZHANG Zheng-Wei WU Ping XUE Fang-Ping DU Fu-Qiang ZHU Jian-Hua LI Cong CHEN Jian GUAN Yi-Hui

摘要： Extensive accumulation of neurofibrillary tangles (NFTs) consistently correlate with the degree of cognitive impairment and neuronal circuitry deterioration associated with Alzheimers disease. However, no PET probe is currently available for selective detection of NFTs in the living human brain. [18F]-THK523 was developed as a potential in vivo imaging probe for tau pathology. In this paper, we report a new protected precursor, 2-((2-(4-(( tert-butoxycarbonyl)amino)phenyl)quinolin-6-yl)oxy)ethyl 4-methylbenzenesulfonate (THK-7), instead of 2-((2-(4-aminophenyl)quinolin-6-yl)oxy)ethyl 4-methylbenzenesulfonate (BF241), and an improved automated radiosynthesis of [18F]-THK523 and the study on chemical kinetics of the labeling reaction of [18F]-THK523, with high-yield (705%, n=6, decay-corrected to end of bombardment), and high radiochemical purity (>90%) and specific activity (2.5 0.5 Ci/mol) from protected precursor on fully automated module at the end of radiosynthesis (4555 min). The chemical kinetics for [18F]-THK523 demonstrates that nucleophilic substitution can be carried out easily with protected precursor.

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