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Automated Radiochemical Synthesis of [18F]3F4AP: A Novel PET Tracer for Imaging Demyelinating Diseases
Published on: May 29, 2017
Fully automated synthesis of [18F]fluorocholine on GE FASTlab II synthesizer
Min Wang1, Chase A Arkins1, Scott E Snyder1
1Molecular Imaging Ligand Development Program, Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN, USA.
Abstract:
A reliable and fully automated method for synthesis, purification and formulation of [18F]FCH on the GE FASTlab II utilizing a single-use cassette was reported. The radiosynthesis sequences of [18F]FCH was written based on the two-step, gas phase synthesis methodology. Dibromomethane (DBM) was fluorinated with no-carrier-added [18F]fluoride ion, assisted by K222/K2CO3, to afford [18F]fluorobromomethane ([18F]FBM) as a gas. [18F]FCH was then prepared by bubbling [18F]FBM through Sep-Pak Silica cartridges to react with dimethylethanolamine (DMAE) preloaded on Sep-Pak C18 cartridge. The resulting [18F]FCH was purified using Sep-Pak C18 and Accell CM cartridges in series. The purified [18F]FCH was eluted from the CM cartridge and formulated with 0.9 % sodium chloride for injection. With this method, the radiochemical yield of [18F]FCH was 17.8 ± 2.5 % with a high radiochemical purity (>99 %). Three consecutive [18F]FCH validation runs were performed, and all quality control parameters met the release criteria for human use. This method is quite straightforward utilizing single-use cassettes. [18F]FCH was reproducibly produced at sufficiently high radioactive concentration for multiple preclinical or human imaging doses from a single radiosynthesis.

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