PROCÉDÉ DE PRÉPARATION DE PRODUITS RADIOPHARMACEUTIQUES SUBSTITUÉS PAR FLUOROMÉTHYLE MARQUÉS AU FLUOR 18 À L'AIDE D'UNE RÉACTION DE SUBSTITUTION D'AZIDE SÉLECTIVE ET D'UN PIÉGEAGE DE PRÉCURSEUR
The present invention relates to a method for preparing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical using selective azide substitution reaction, the method comprising: a first step for obtaining [18F]fluoride from a cyclotron through a 18O(p, n)18F reaction； a second step for obtaining a [18F]F-/H218O solution by separating the [18F]fluoride using an acetonitrile reaction solution in which K2.2.2 and K2CO3 are dissolved； a third step for obtaining K2.2.2/K18F by heating the [18F]F-/H218O solution； a fourth step for obtaining a first precursor solution by adding the K2.2.2/K18F and a bistoxyloxymethane compound into a reactor and adding a reaction solvent thereto to cause reaction； a fifth step for obtaining a [18F]fluoromethyltosylate compound by cooling the first precursor solution and adding an azide reagent thereto to cause azide substitution reaction； a sixth step for obtaining a second precursor solution by adding a bioactive molecule precursor to the [18F]fluoromethyltosylate compound to cause alkylation reaction； and a seventh step for preparing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical without a HPLC separation process by adding a precursor scavenger to the second precursor solution to remove unreacted precursors. According to the present invention, in the synthesis process of a radiopharmaceutical, by non-activating an excess amount of a bistoxyloxymethane compound present in a reaction mixture through selective azide substitution reaction and remarkably enhancing a yield of alkylation between the bioactive molecule precursor and the [18F]fluoromethyltosylate compound in the subsequent step, a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical with high radiochemical purity can be synthesized even when HPLC separation and purification processes are omitted, and thus manufacturing time and manufacturing costs due to the HPLC process can be reduced.La présente invention concerne un procédé de prép
