title: Automated synthesis of N-(2-[18F]Fluoropropionyl)-l-glutamic acid as an amino acid tracer for tumor imaging on a modified [18F]FDG synthesis module.
abstract: N-(2-[18F]Fluoropropionyl)-l-glutamic acid ([18F]FPGLU) is a potential amino acid tracer for tumor imaging with positron emission tomography. However, due to the complicated multistep synthesis, the routine production of [18F]FPGLU presents many challenging laboratory requirements. To simplify the synthesis process of this interesting radiopharmaceutical, an efficient automated synthesis of [18F]FPGLU was performed on a modified commercial fluorodeoxyglucose synthesizer via a 2-step on-column hydrolysis procedure, including18F-fluorination and on-column hydrolysis reaction. [18F]FPGLU was synthesized in 12 ± 2% (n = 10, uncorrected) radiochemical yield based on [18F]fluoride using the tosylated precursor 2. The radiochemical purity was ≥98%, and the overall synthesis time was 35 minutes. To further optimize the radiosynthesis conditions of [18F]FPGLU, a brominated precursor 3 was also used for the preparation of [18F]FPGLU, and the improved radiochemical yield was up to 20 ± 3% (n = 10, uncorrected) in 35 minutes. Moreover, all these results were achieved using the similar on-column hydrolysis procedure on the modified fluorodeoxyglucose synthesis module.
authors.affiliation: School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.|Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Shaoyu
authors.initials: S
authors.lastname: Liu
authors.affiliation: Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Aixia
authors.initials: A
authors.lastname: Sun
authors.affiliation: Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Zhanwen
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: School of materials and energy, South China Agricultural University, Guangzhou, China.
authors.forename: Xiaolan
authors.initials: X
authors.lastname: Tang
authors.affiliation: Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Dahong
authors.initials: D
authors.lastname: Nie
authors.affiliation: Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Ma
authors.affiliation: School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.
authors.forename: Shende
authors.initials: S
authors.lastname: Jiang
authors.affiliation: Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, SunYat-sen University, Guangzhou, China.
authors.forename: Ganghua
authors.identifier: 0000-0003-2639-0388
authors.initials: G
authors.lastname: Tang
mesh_terms: D001331:Automation; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D019788:Fluorodeoxyglucose F18 / Q000138:chemical synthesis* / Q000737:chemistry; D005971:Glutamates / Q000138:chemical synthesis* / Q000737:chemistry; D006868:Hydrolysis; D007700:Kinetics; D009369:Neoplasms / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers
chemical_list: D005971:Glutamates; C000603314:N-(2-fluoropropionyl)glutamic acid; D011849:Radioactive Tracers; D019788:Fluorodeoxyglucose F18
keywords: [18F]FPGLU; amino acid tracer; automated synthesis; precursor synthesis