title: Improved synthesis of [(18)F]FLETT via a fully automated vacuum distillation method for [(18)F]2-fluoroethyl azide purification.
abstract: The synthesis of [(18)F]2-fluoroethyl azide and its subsequent click reaction with 5-ethynyl-2'-deoxyuridine (EDU) to form [(18)F]FLETT was performed using an iPhase FlexLab module. The implementation of a vacuum distillation method afforded [(18)F]2-fluoroethyl azide in 87±5.3% radiochemical yield. The use of Cu(CH3CN)4PF6 and TBTA as catalyst enabled us to fully automate the [(18)F]FLETT synthesis without the need for the operator to enter the radiation field. [(18)F]FLETT was produced in higher overall yield (41.3±6.5%) and shorter synthesis time (67min) than with our previously reported manual method (32.5±2.5% in 130min).
authors.affiliation: Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, VIC, Australia; The University of Melbourne, Parkville, VIC, Australia; Ludwig Institute for Cancer Research, Melbourne Branch, VIC, Australia.
authors.forename: Uwe
authors.initials: U
authors.lastname: Ackermann
authors.affiliation: Ecole National Supérior de Chimie de Rennes, Rennes, France.
authors.forename: Lucie
authors.initials: L
authors.lastname: Plougastel
authors.affiliation: Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, VIC, Australia; The University of Melbourne, Parkville, VIC, Australia.
authors.forename: Yit Wooi
authors.initials: YW
authors.lastname: Goh
authors.affiliation: Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, VIC, Australia; The University of Melbourne, Parkville, VIC, Australia.
authors.forename: Shinn Dee
authors.initials: SD
authors.lastname: Yeoh
authors.affiliation: Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, VIC, Australia; The University of Melbourne, Parkville, VIC, Australia; Ludwig Institute for Cancer Research, Melbourne Branch, VIC, Australia.
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Scott
mesh_terms: D001386:Azides / Q000138:chemical synthesis* / Q000302:isolation & purification*; D057168:Distillation / Q000295:instrumentation* / Q000379:methods; D004867:Equipment Design; D019544:Equipment Failure Analysis; D005462:Fluorine Radioisotopes / Q000737:chemistry* / Q000302:isolation & purification*; D007553:Isotope Labeling / Q000295:instrumentation* / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000302:isolation & purification; D012371:Robotics / Q000295:instrumentation / Q000379:methods*; D014618:Vacuum
chemical_list: C522266:2-fluoroethylazide; D001386:Azides; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals
keywords: Automation; Click chemistry; Fluorine-18; Vacuum distillation