Automated synthesis and purification of [18F]fluoro-[di-deutero]methyl tosylate

Abstract

Automated synthetic procedures of [(18)F]fluoro-[di-deutero]methyl tosylate on a GE TRACERlab FX F-N module and a non-commercial synthesis module have been developed. The syntheses included azeotropic drying of the [(18)F]fluoride, nucleophilic (18)F-fluorination of bis(tosyloxy)-[di-deutero]methane, HPLC purification and subsequent formulation of the synthesized [(18)F]fluoro-[di-deutero]methyl tosylate (d2-[(18)F]FMT) in organic solvents. Automation shortened the total synthesis time to 50 min, resulting in an average radiochemical yield of about 50% and high radiochemical purity (>98%). The possible application of this procedure to commercially available synthesis modules might be of significance for the production of deuterated (18)F-fluoromethylated imaging probes in the future.

Keywords: 18F-fluoromethylation; PET; [18F]fluorine; [18F]fluoromethyl tosylate; automated synthesis.