title: Continuous-Flow Synthesis of N-Succinimidyl 4-[18F]fluorobenzoate Using a Single Microfluidic Chip.
abstract: In the field of positron emission tomography (PET) radiochemistry, compact microreactors provide reliable and reproducible synthesis methods that reduce the use of expensive precursors for radiolabeling and make effective use of the limited space in a hot cell. To develop more compact microreactors for radiosynthesis of 18F-labeled compounds required for the multistep procedure, we attempted radiosynthesis of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) via a three-step procedure using a microreactor. We examined individual steps for [18F]SFB using a batch reactor and microreactor and developed a new continuous-flow synthetic method with a single microfluidic chip to achieve rapid and efficient radiosynthesis of [18F]SFB. In the synthesis of [18F]SFB using this continuous-flow method, the three-step reaction was successfully completed within 6.5 min and the radiochemical yield was 64 ± 2% (n = 5). In addition, it was shown that the quality of [18F]SFB synthesized on this method was equal to that synthesized by conventional methods using a batch reactor in the radiolabeling of bovine serum albumin with [18F]SFB.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.|Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Kyoto, Kyoto, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Kimura
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.
authors.forename: Kenji
authors.initials: K
authors.lastname: Tomatsu
authors.affiliation: Technology Research Laboratory, Shimadzu Corporation, Souraku-gun, Kyoto, Japan.
authors.forename: Hidekazu
authors.initials: H
authors.lastname: Saiki
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.|School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Hyogo, Japan.
authors.forename: Kenji
authors.initials: K
authors.lastname: Arimitsu
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.
authors.forename: Masahiro
authors.initials: M
authors.lastname: Ono
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.|Radioisotope Research Center, Kyoto Pharmaceutical University, Kyoto, Kyoto, Japan.
authors.forename: Hidekazu
authors.initials: H
authors.lastname: Kawashima
authors.affiliation: CYRIC, Tohoku University, Sendai, Miyagi, Japan.
authors.forename: Ren
authors.initials: R
authors.lastname: Iwata
authors.affiliation: Technology Research Laboratory, Shimadzu Corporation, Souraku-gun, Kyoto, Japan.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Nakanishi
authors.affiliation: Technology Research Laboratory, Shimadzu Corporation, Souraku-gun, Kyoto, Japan.
authors.forename: Eiichi
authors.initials: E
authors.lastname: Ozeki
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.|Central Institute of Isotope Science, Hokkaido University, Sapporo, Hokkaido, Japan.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Kuge
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Kyoto, Japan.
authors.forename: Hideo
authors.initials: H
authors.lastname: Saji
mesh_terms: D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D044085:Microfluidics / Q000379:methods*; D049268:Positron-Emission Tomography / Q000379:methods*; D011854:Radiochemistry / Q000379:methods; D019275:Radiopharmaceuticals / Q000737:chemistry; D013388:Succinimides / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D001565:Benzoates; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D013388:Succinimides; C075713:N-succinimidyl-4-fluorobenzoate