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

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 2.5 h.

Graphical AbstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Automated production of [18F]gefitinib on a commercially available modular system. ► 3-Step synthesis provides [18F]gefitinib in 17.2±3.3 % radiochemical yield. ► Radiochemical purity at the end of synthesis was >99% (n=22).