公开(公告)号：US12274760B2

公开(公告)日：2025-04-15

申请号：US17206979

申请日：2021-03-19

Applicant: Byung Chul Lee

Inventor： Byung Chul Lee ,  Ying Qing Lu ,  Byeong Min Jo

IPC: A61K51/04

Abstract: 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 K2,2,2 and K2CO3 to obtain a [18F]F−/H218O solution; (3) heating the [18F]F−/H218O solution to obtain K2,2,2/K18F; (4) placing the K2,2,2/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.