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

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]-...

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Published in:核技术（英文版） 2014-08, Vol.25 (4), p.28-35
Main Author: 孔艳艳 司展 曹国宪 张政伟 吴平 薛方平 杜富强 朱建华 李聪 陈键 管一晖
Format: Article
Language:English
Subjects:
PET探测器
全自动化
制备工艺
化学动力学
合成
成像
放射化学纯度
阿尔茨海默氏病
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Summary: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 of2-（（2-（4-aminophenyl）quinolin-6-yl）oxy）ethyl 4-methylbenzenesulfonate（BF241）,and an improved automated radiosynfhesis 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 ± 0.5Ci/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.
ISSN:1001-8042
2210-3147
DOI:10.13538/j.1001-8042/nst.25.040302