Full automatic synthesis of [18F]THK-5351 for tau protein PET imaging in Alzheimer’s disease patients: 1 year experience

Sang Ju Lee; Seung Jun Oh; Eun Hye Cho; Da Hye Kim; Shozo Furumoto; Nobuyuki Okamura; Jae Seung Kim

doi:10.1007/s10967-017-5573-7

Full automatic synthesis of [¹⁸F]THK-5351 for tau protein PET imaging in Alzheimer’s disease patients: 1 year experience

Sang Ju Lee, Seung Jun Oh, Eun Hye Cho, Da Hye Kim, Shozo Furumoto, Nobuyuki Okamura, Jae Seung Kim

Cyclotron and Radioisotope Center (CYRIC)

Research output: Contribution to journal › Article › peer-review

Abstract

[¹⁸F]THK-5351, a new candidate for tau protein imaging, is based on an aryl quinoline structure. We report the full automatic synthesis using disposable cassettes under pH controlled [¹⁸F]fluorination. After the trapping of 88.5 ± 21.9 GBq of [¹⁸F]fluoride, it was eluted with potassium methansulfonate (KOMs) (pH 7.8)/K₂₂₂. After drying, 3 mg of the precursor was added to 1 mL DMSO and subjected to [¹⁸F]fluorination at 110 °C for 10 min. After hydrolysis, the final product was purified by HPLC. The overall radiochemical yield was 31.9 ± 11.1% (n = 22), satisfying all quality control criteria. It was stable for up to 6 h with high radiochemical purity as 99.8 ± 0.5%.

Original language	English
Pages (from-to)	1587-1593
Number of pages	7
Journal	Journal of Radioanalytical and Nuclear Chemistry
Volume	314
Issue number	3
DOIs	https://doi.org/10.1007/s10967-017-5573-7
Publication status	Published - 2017 Dec 1

Keywords

Automatic synthesis
PET imaging
Tau protein positron emission tomography
THK-5351
[F]fluorination

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1007/s10967-017-5573-7

Cite this

@article{38c3094406f94a56bd2da22969ca498e,

title = "Full automatic synthesis of [18F]THK-5351 for tau protein PET imaging in Alzheimer{\textquoteright}s disease patients: 1 year experience",

abstract = "[18F]THK-5351, a new candidate for tau protein imaging, is based on an aryl quinoline structure. We report the full automatic synthesis using disposable cassettes under pH controlled [18F]fluorination. After the trapping of 88.5 ± 21.9 GBq of [18F]fluoride, it was eluted with potassium methansulfonate (KOMs) (pH 7.8)/K222. After drying, 3 mg of the precursor was added to 1 mL DMSO and subjected to [18F]fluorination at 110 °C for 10 min. After hydrolysis, the final product was purified by HPLC. The overall radiochemical yield was 31.9 ± 11.1% (n = 22), satisfying all quality control criteria. It was stable for up to 6 h with high radiochemical purity as 99.8 ± 0.5%.",

keywords = "Automatic synthesis, PET imaging, Tau protein positron emission tomography, THK-5351, [F]fluorination",

author = "Lee, {Sang Ju} and Oh, {Seung Jun} and Cho, {Eun Hye} and Kim, {Da Hye} and Shozo Furumoto and Nobuyuki Okamura and Kim, {Jae Seung}",

note = "Funding Information: Acknowledgements This work was supported by a grant from the Korea Health Technology R&D Project through the Korea Health Publisher Copyright: {\textcopyright} 2017, Akad{\'e}miai Kiad{\'o}, Budapest, Hungary.",

year = "2017",

month = dec,

day = "1",

doi = "10.1007/s10967-017-5573-7",

language = "English",

volume = "314",

pages = "1587--1593",

journal = "Journal of Radioanalytical and Nuclear Chemistry",

issn = "0236-5731",

publisher = "Springer Netherlands",

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TY - JOUR

T1 - Full automatic synthesis of [18F]THK-5351 for tau protein PET imaging in Alzheimer’s disease patients

T2 - 1 year experience

AU - Lee, Sang Ju

AU - Oh, Seung Jun

AU - Cho, Eun Hye

AU - Kim, Da Hye

AU - Furumoto, Shozo

AU - Okamura, Nobuyuki

AU - Kim, Jae Seung

N1 - Funding Information: Acknowledgements This work was supported by a grant from the Korea Health Technology R&D Project through the Korea Health Publisher Copyright: © 2017, Akadémiai Kiadó, Budapest, Hungary.

PY - 2017/12/1

Y1 - 2017/12/1

N2 - [18F]THK-5351, a new candidate for tau protein imaging, is based on an aryl quinoline structure. We report the full automatic synthesis using disposable cassettes under pH controlled [18F]fluorination. After the trapping of 88.5 ± 21.9 GBq of [18F]fluoride, it was eluted with potassium methansulfonate (KOMs) (pH 7.8)/K222. After drying, 3 mg of the precursor was added to 1 mL DMSO and subjected to [18F]fluorination at 110 °C for 10 min. After hydrolysis, the final product was purified by HPLC. The overall radiochemical yield was 31.9 ± 11.1% (n = 22), satisfying all quality control criteria. It was stable for up to 6 h with high radiochemical purity as 99.8 ± 0.5%.

AB - [18F]THK-5351, a new candidate for tau protein imaging, is based on an aryl quinoline structure. We report the full automatic synthesis using disposable cassettes under pH controlled [18F]fluorination. After the trapping of 88.5 ± 21.9 GBq of [18F]fluoride, it was eluted with potassium methansulfonate (KOMs) (pH 7.8)/K222. After drying, 3 mg of the precursor was added to 1 mL DMSO and subjected to [18F]fluorination at 110 °C for 10 min. After hydrolysis, the final product was purified by HPLC. The overall radiochemical yield was 31.9 ± 11.1% (n = 22), satisfying all quality control criteria. It was stable for up to 6 h with high radiochemical purity as 99.8 ± 0.5%.

KW - Automatic synthesis

KW - PET imaging

KW - Tau protein positron emission tomography

KW - THK-5351

KW - [F]fluorination

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