A radiolabeled amino acid O-[F]fluoromethyl-D-tyrosine (D-[F]FMT) has been reported to show high tumor uptake. However, introduction of [F]fluoromethyl group was difficult and was an issue to be solved. We solved it by using a precursor containing 1,2,3-triazolium salt. D-[F]FMT was synthesized from (R)-1-((4-(2-((tert-butoxycarbonyl)amino)-3-((3,4-dimethylbenzyl)oxy)-3-oxopropyl)phenoxy)methyl)-3-methyl-4-phenyl-1H-1,2,3-triazol-3-ium trifluoromethanesulfonate via intra-molecular F-fluorination and subsequent removal of the protecting groups. The total synthesis time was 65min (including purification) and the overall radiochemical yield was 9% based on the isolated product (not decay-corrected). The resulting D-[F]FMT was obtained with high radiochemical purity (> 99%) and specific activity (100-150 GBq/μmol). D-[F]FMT also achieved excellent results in pharmacological evaluation such as stability test and protein binding assay. We expect that this simple one-pot labeling method would help using D-[F]FMT more widely.
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