121st General Meeting of the KCS

Type Poster Presentation
Area Organic Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code ORGN.P-374
Subject Azeotropic drying-free aliphatic radiofluorination to produce PET radiotracers in mixed organic solvents
Authors Young-Do Kwon, JEONGMIN SON1, Mijin Yun, Joong-Hyun Chun*
Department of Nuclear Medicine, Yonsei University College of Medicine, Korea
1Department of Nuclear Medicine, Yonsei University Health System, Korea
Abstract Positron emission tomography (PET), which is a well-established non-invasive molecular imaging modality, provides valuable information on the biochemical process associated with radiotracers in vivo. Fluorine-18 is the radionuclide of choice for PET imaging in this regard, due to its ideal imaging properties such as low positron energy and clean decay process. It has been known that the nucleophilicity of [18F]fluoride ion is adversely affected by degrees of hydration with water. This often leads to detrimental radiofluorination outcome. To overcome this limitation, the time-consuming (10 ~ 20 min) azeotropic drying process has been routinely used in order to completely remove water from aqueous medium. In addition, a condensed radiolabeling process is required to achieve the successful imaging studies with PET, considering short physical half-live (t1/2 = 110 min.) of fluorine-18. Herein, we developed a streamlined radiofluorination method omitting azeotropic drying process, using [18F]fluoride ion directly eluted from QMA with phase transfer agent. The reactions were preceded in mixed organic solvents. Various clinical radiotracers, such as [18F]PSS232, [18F]FMISO, and [18F]fallypride were demonstrated to provide 12 ~ 46 % RCYs. The results obtained from PET radiotracer suggest that the azeotropic drying-free method would be a potentially efficient aliphatic radiofluorination protocol, especially advantageous for convenient optimization of radiochemistry for newly developed PET radiopharmaceuticals. This work was supported by the National Research Foundation (NRF) of Korea, funded by the Ministry of Science, ICT & Future Planning (NRF-2015R1D1A1A02061420, 2015K1A3A1A14021182).
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