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Appl Radiat Isot. 2000 Jan;52(1):55-61.

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

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Department of Radiology, Case Western Reserve University and University Hospitals of Cleveland, OH 44106, USA.


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


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