Automated Synthesis of ~(18)F-Labelled Fluoromisonidazole as Hypoxia Imaging Agent

H-1-(3-~(18)F-fluoro-2-hydroxylpropyl)-2-nitroimidazole(~(18)F-FMISO) is synthesized by “one pot” method at Tracerlab FX_(F-N) system. By using 1-(2’-nitro-1’-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonyl-propanediol as the precursor, ~(18)F-FMISO is obtained via two-step reactions, including the nucleophilic fluoration of the precursor to yield an intermediate 1-(2’-nitro-1’-imidazolyl)-2-O-tetrahydropyranyl)-3-~(18)F-fluoropropanol, and the acidic hydrolysis of the intermediate. The procedure is guite simple and can be completed within 60 min. The radiochemical yield and radiochemical purity are higher than 60% and 99%, respectively. Toxicological assays indicate that the final product is bacteria-free and non-toxic, and meets the requirements for radiopharmacy. It can be used in clinical and scientific research.