Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2014, Vol. 25 ›› Issue (4): 040302 doi: 10.13538/j.1001-8042/nst.25.040302

• NUCLEAR CHEMISTRY,RADIOCHEMISTRY,RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

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

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   

  1. 1PET Center, Huashan Hospital, Fudan University, Shanghai 200235, China
    2Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
    3Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, School of Pharmacy, Fudan University, Shanghai 200032, China
  • Contact: GUAN Yi-Hui E-mail:guanyihui@hotmail.com
  • Supported by:

    Supported by National Natural Science Foundation of China (Nos. 81271516 and 81371625), Program of Shanghai Science and Technology Commission (Nos. 13JC1401503 and 14DZ1930402), the exchange program fund of doctoral student under the office for Graduate Medical Education, Fudan University and Shanghai Municipal Health and Family Planning Commission (No. 2013313)

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KONG Yan-Yan, SI Zhan, CAO Guo-Xian, ZHANG Zheng-Wei, WU Ping, XUE Fang-Ping, DU Fu-Qiang, . Improved preparation and chemical kinetics on fully automated synthesis of [18F]-THK523, a PET imaging probe for Tau pathologies.Nuclear Science and Techniques, 2014, 25(4): 040302     doi: 10.13538/j.1001-8042/nst.25.040302

Abstract:

Extensive accumulation of neurofibrillary tangles (NFTs) consistently correlate with the degree of cognitive impairment and neuronal circuitry deterioration associated with Alzheimer’s 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 (70 ± 5%, n = 6, decay-corrected to end of bombardment), and high radiochemical purity (> 90%) and specific activity (2:5  0:5 Ci/μmol) from protected precursor on fully automated module at the end of radiosynthesis (45–55 min). The chemical kinetics for [18F]-THK523 demonstrates that nucleophilic substitution can be carried out easily with protected precursor.

Key words: Fluorine-18 radiolabeling, Neurofibrillary tangles, Alzheimer’s disease, Automated radiosynthesis, Chemical kinetics