Automated Synthesis of ¹⁸F-Labelled FAZA as Hypoxia Imaging Agent

1-(5-［¹⁸F］fluoro-5-deoxy-α-D-arabinofuranosyl)-2-nitroimidazole was synthesized by “two pot” method at a multifunctional CPCU made in China and by using 1-(2,3-di-O-acetyl-5-O-tosyl-α-D-arabinofuranosyl)-2-nitroimidazole as precursor. The precursor (4-6 mg) was fluorinated at 115℃ for 10min. The F-18 labeled intermediate was traped by a C-18 column, then was hydrolyzed using NaOH. The reaction mixture was neutralized by adding HCl, and was purified through HPLC. The pure ¹⁸FAZA is obtained for no more than 45 min. The overall radiochemical yield is more than 10%, and the radiopurity is higher than 98%. ¹⁸FAZA is successfully autosynthesized through “two pot” method. It can be used in clinical and scientific research.