title: Development of a resonant-type microwave reactor and its application to the synthesis of positron emission tomography radiopharmaceuticals.
abstract: Microwave technology has been successfully applied to enhance the effectiveness of radiolabeling reactions. The use of a microwave as a source of heat energy can allow chemical reactions to proceed over much shorter reaction times and in higher yields than they would do under conventional thermal conditions. A microwave reactor developed by Resonance Instrument Inc. (Model 520/521) and CEM (PETWave) has been used exclusively for the synthesis of radiolabeled agents for positron emission tomography by numerous groups throughout the world. In this study, we have developed a novel resonant-type microwave reactor powered by a solid-state device and confirmed that this system can focus microwave power on a small amount of reaction solution. Furthermore, we have demonstrated the rapid and facile radiosynthesis of 16α-[(18)F]fluoroestradiol, 4-[(18)F]fluoro-N-[2-(1-methoxyphenyl)-1-piperazinyl]ethyl-N-2-pyridinylbenzamide, and N-succinimidyl 4-[(18)F]fluorobenzoate using our newly developed microwave reactor.
authors.affiliation: Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto, Kyoto, 606-8501, Japan; Radioisotope Research Center, Kyoto University, Yoshida Konoe-cho, Sakyo-ku, Kyoto, Kyoto, 606-8501, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Kimura
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Yagi
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Ohneda
authors.forename: Hiro
authors.initials: H
authors.lastname: Odajima
authors.forename: Masahiro
authors.initials: M
authors.lastname: Ono
authors.forename: Hideo
authors.initials: H
authors.lastname: Saji
mesh_terms: D001565:Benzoates / Q000138:chemical synthesis*; D060326:Chemistry Techniques, Synthetic / Q000295:instrumentation* / Q000379:methods; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D008872:Microwaves; D010879:Piperazines / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography; D011725:Pyridines / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D013388:Succinimides / Q000138:chemical synthesis*
chemical_list: C114151:4-fluoro-N-(2-(1-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-2-pyridinylbenzamide; D001565:Benzoates; D010879:Piperazines; D011725:Pyridines; D019275:Radiopharmaceuticals; D013388:Succinimides; C075713:N-succinimidyl-4-fluorobenzoate; D004958:Estradiol; C043436:16-fluoroestradiol
keywords: 18F-fluorination; [18F]FES; [18F]MPPF; [18F]SFB; positron emission tomography radiochemistry; resonant-type microwave reactor