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

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

doi:10.13538/j.1001-8042/nst.25.040302

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

NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE | Updated：2021-01-20

- Improved preparation and chemical kinetics on fully automated synthesis of [¹⁸F]-THK523, a PET imaging probe for Tau pathologies
- Nuclear Science and Techniques Vol. 25, Issue 4, Article number: 040302(2014)
- Affiliations：
  
  1.PET Center, Huashan Hospital, Fudan University, Shanghai200235, China
  2.Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi214063, China
  3.Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, School of Pharmacy, Fudan University, Shanghai200032, China
- Author bio：
  
  Corresponding author,guanyihui@hotmail.com
- Funds：
- DOI：10.13538/j.1001-8042/nst.25.040302
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Yan-Yan KONG, Zhan SI, Guo-Xian CAO, et al. Improved preparation and chemical kinetics on fully automated synthesis of [¹⁸F]-THK523, a PET imaging probe for Tau pathologies. [J]. Nuclear Science and Techniques 25(4):040302(2014)
DOI：

Yan-Yan KONG, Zhan SI, Guo-Xian CAO, et al. Improved preparation and chemical kinetics on fully automated synthesis of [¹⁸F]-THK523, a PET imaging probe for Tau pathologies. [J]. Nuclear Science and Techniques 25(4):040302(2014) DOI： 10.13538/j.1001-8042/nst.25.040302.

摘要

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. [,18,F]-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 [,18,F]-THK523 and the study on chemical kinetics of the labeling reaction of [,18,F]-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 [,18,F]-THK523 demonstrates that nucleophilic substitution can be carried out easily with protected precursor.

关键词

Keywords

Fluorine-18 radiolabelingNeurofibrillary tanglesAlzheimer’s diseaseAutomated radiosynthesisChemical kinetics

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Key Laboratory of Nuclear Medicine, Ministry of Health

Key Laboratory of Molecular Nuclear Medicine of Jiangsu

Jiangsu Institute of Nuclear Medicine

Nuclear Safety Group, Nuclear Engineering Department, Xi'an Jiaotong University

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

DOI：10.13538/j.1001-8042/nst.25.040302

摘要

Abstract

关键词

Keywords

references

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