Radiosynthesis and preliminary biological evaluation of the 2-[18F]fluoropropionic acid enantiomers for tumor PET imaging |
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| Authors: | Zhanwen Zhang Shaoyu Liu Xiaolan Tang Dahong Nie Ganghua Tang Aixia Sun Ying Xiong Hui Ma Fuhua Wen Ping Hu |
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| Affiliation: | 1.Department of Nuclear Medicine, Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, The First Affiliated Hospital,Sun Yat-Sen University,Guangzhou,China;2.Department of Nuclear Medicine,The Sixth Affiliated Hospital,Sun Yat-Sen University,Guangzhou,China;3.School of Materials and Energy,South China Agricultural University,Guangzhou,China |
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| Abstract: | The aim of this study was to synthesize the optically pure [18F]FPA, and to investigate the diagnostic value of different isomers. Semi-automated radiosynthesis of R-[18F]FPA or S-[18F]FPA was respectively from the chiral precursor (S)- or (R)-ethyl 2-(((trifluoromethyl)sulfonyl)oxy)propanoate via a two-step reaction and performed on the commercial FDG synthesizer. The improved radiochemical yields of R-[18F]FPA and S-[18F]FPA were 30–40% (decay-uncorrected, n = 10) in 35 min. There was no significant difference on the biodistribution of two enantiomers in normal mice (P > 0.05), but positron emission tomography imaging demonstrated that R-[18F]FPA was more suitable for PC3 tumor imaging than S-[18F]FPA and [18F]FDG. |
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