METHOD FOR PREPARING FLUORINE-18-LABELED FLUOROMETHYL-SUBSTITUTED RADIOPHARMACEUTICALS USING SELECTIVE AZIDE SUBSTITUTION REACTION AND PRECURSOR SCAVENGING

摘要

A method for preparing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical using a selective azide substitution reaction includes (1) obtaining a [¹⁸F]fluoride from a cyclotron through an ¹⁸O(p,n)¹⁸F reaction; (2) separating the [¹⁸F] fluoride using an acetonitrile reaction solution containing dissolved K_2,2,2 and K₂CO₃ to obtain a [¹⁸F]F⁻/H₂¹⁸O solution; (3) heating the [¹⁸F]F⁻/H₂¹⁸O solution to obtain K_2,2,2/K¹⁸F; (4) placing the K_2,2,2/K¹⁸F along with a bis(tosyloxy)methane compound into a reactor and adding a reaction solvent to cause a reaction and obtain a first precursor solution; (5) cooling the first precursor solution and adding an azide reagent to cause an azide substitution reaction and obtain a [¹⁸F]fluoromethyltosylate compound; (6) adding a bioactive molecule to the [¹⁸F]fluoromethyltosylate compound to cause an alkylation reaction and obtain a second precursor solution; and (7) adding a precursor scavenger to the second precursor solution and scavenging unreacted precursors to produce a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical.