Synthesis of [18F]fluoromethyl iodide, a synthetic precursor for fluoromethylation of radiopharmaceuticals

[F-18]fluoroiodomethane was labeled via nucleophilic substitution of diiodomethane with [F-18]fluoride, and labeling conditions were optimized. The optimized labeling yield was 40 +/- 8% (decay-corrected). The synthesis and purification of [F-18]fluoroiodomethane took 15 min. The reactions of [F-18]fluoroiodomethane with amine, carboxylic acid, thiol and phenoxide groups produced fluoromethylated derivatives with various yields (12-95%). The results indicated that [F-18]fluoroiodomethane is a valuable synthetic precursor for the introduction of an [F-18]fluoromethyl group into radiopharmaceuticals. (C) 2000 Published by Elsevier Science Ltd. All rights reserved.