Improved preparation and chemical kinetics on fully automated synthesis of [18F]-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

Research output: Contribution to journalArticle

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/?mol) 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.

Original languageEnglish (US)
Article number040302
JournalNuclear Science and Techniques
Volume25
Issue number4
DOIs
StatePublished - Jul 4 2014
Externally publishedYes

Fingerprint

quinoline
pathology
Pathology
Reaction kinetics
reaction kinetics
Imaging techniques
preparation
probes
impairment
kinetics
synthesis
deterioration
Labeling
marking
brain
Deterioration
bombardment
Brain
purity
Substitution reactions

Keywords

  • Alzheimer's disease
  • Automated radiosynthesis
  • Chemical kinetics
  • Fluorine-18 radiolabeling
  • Neurofibrillary tangles

ASJC Scopus subject areas

  • Nuclear Energy and Engineering
  • Nuclear and High Energy Physics

Cite this

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.

In: Nuclear Science and Techniques, Vol. 25, No. 4, 040302, 04.07.2014.

Research output: Contribution to journalArticle

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. / Improved preparation and chemical kinetics on fully automated synthesis of [18F]-THK523, a PET imaging probe for Tau pathologies. In: Nuclear Science and Techniques. 2014 ; Vol. 25, No. 4.
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