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A New Method Using Anhydrous [¹⁸F]fluorine to Radiolabel 2-[¹⁸F]Fluoro-2-Deoxy-D-Glucose

Massachusetts General Hospital, Boston, Massachusetts

Correspondence: For reprints contact: D. R. Elmaleh, Physics Research Laboratory, Massachusetts General Hospital, Boston, MA 02114.

ABSTRACT

We report a new chemical route for the preparation of 2-[¹⁸F]fluoro-2-deoxy-D-glucose (2-¹⁸FDG) using anhydrous [¹⁸F]fluoride produced by the ²⁰Ne(d,)¹⁸F reaction. The anhydrous ¹⁸F– is reacted with a previously prepared precursor, methyl 4,6-o-benzylidene-3-o-methyl-2-O-trifluoromethanesulfonyt-ß-D-mannopyranoside, in dimethyl formamide or hexamethylphosphoric triamide. The corresponding fluoro-deoxy-glucose derivative, upon treatment with borontribromide or concentrated hydrochloric acid, yields 2-¹⁸FDG in 10% (overall) yeild. The substrate was characterized by thin-layer chromatography (TLC), and high-performance liquid chromatography (HPLC). Biodistribution studies were performed in mice, and imaging studies in dogs.