title: Automated synthesis of [18F]gefitinib on a modular system.
abstract: In recent years, [(18)F]gefitinib PET has successfully been employed for a number of applications ranging from oncology to in vivo studies of drug transporter proteins. We here report a reliable, automated procedure for routine synthesis of this radiotracer on an Eckert and Ziegler modular system. The 3-step radiosynthesis followed by preparative HPLC-purification provided [(18)F]gefitinib in 17.2±3.3% (n=22) overall decay-corrected radiochemical yield with radiochemical purity >99% in a total synthesis time of about 2.5h.
authors.affiliation: Philips Research Europe, Department of Biomolecular Engineering, High Tech Campus 11, 5656 AE Eindhoven, The Netherlands. tilman.lappchen@philips.com
authors.forename: Tilman
authors.initials: T
authors.lastname: Läppchen
authors.forename: Maria L H
authors.initials: ML
authors.lastname: Vlaming
authors.forename: Erica
authors.initials: E
authors.lastname: Custers
authors.forename: Johan
authors.initials: J
authors.lastname: Lub
authors.forename: Charles F
authors.initials: CF
authors.lastname: Sio
authors.forename: Jeroen
authors.initials: J
authors.lastname: DeGroot
authors.forename: Oliver C
authors.initials: OC
authors.lastname: Steinbach
mesh_terms: D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation*; D004867:Equipment Design; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D000077156:Gefitinib; D007553:Isotope Labeling / Q000295:instrumentation*; D011799:Quinazolines / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D012371:Robotics / Q000295:instrumentation*
chemical_list: D005462:Fluorine Radioisotopes; D011799:Quinazolines; D019275:Radiopharmaceuticals; D000077156:Gefitinib