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Automated synthesis of [18F]gefitinib on a modular system

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Author: Läppchen, T. · Vlaming, M.L.H. · Custers, E. · Lub, J. · Sio, C.F. · DeGroot, J. · Steinbach, O.C.
Type:article
Date:2012
Source:Applied Radiation and Isotopes, 1, 70, 205-209
Identifier: 446406
doi: doi:10.1016/j.apradiso.2011.09.005
Keywords: Biology · Automated synthesis · Imaging of drug transporters · Modular system · PET tracer · Automated procedures · Automated synthesis · Gefitinib · In-vivo · Modular system · PET tracer · Radiochemical purity · Radiochemical yield · Radiosynthesis · Total synthesis · Transporter proteins · Automation · Biosynthesis · gefitinib f 18 · radiopharmaceutical agent · unclassified drug · analytic method · article · automation · drug purification · drug structure · drug synthesis · high performance liquid chromatography · priority journal · quality control · radiochemistry · radioisotope decay · Healthy Living · Life · PHS - Pharmacokinetics & Human Studies · EELS - Earth, Environmental and Life Sciences

Abstract

In recent years, [ 18F]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 [ 18F]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. © 2011 Elsevier Ltd.