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

Appl Radiat Isot. 2012 Jan;70(1):205-9. doi: 10.1016/j.apradiso.2011.09.005. Epub 2011 Sep 17.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chromatography, High Pressure Liquid / instrumentation*
  • Equipment Design
  • Fluorine Radioisotopes / chemistry*
  • Gefitinib
  • Isotope Labeling / instrumentation*
  • Quinazolines / chemical synthesis*
  • Radiopharmaceuticals / chemical synthesis*
  • Robotics / instrumentation*

Substances

  • Fluorine Radioisotopes
  • Quinazolines
  • Radiopharmaceuticals
  • Gefitinib