High yield one-pot production of [18F]FCH via a modified TRACERlab FxFN module
Journal
Applied Radiation and Isotopes
Journal Volume
128
Pages
190-198
Date Issued
2017
Author(s)
Abstract
Introduction [18F]Fluoromethylcholine ([18F]FCH) is a potent tumors imaging agent. In order to fulfill the demand of pre-clinical and clinical studies, we have developed an automated high yield one-pot synthesis of this potent tumors imaging agent. Methods [18F]FCH was synthesized using a modified TRACERlab FxFN module. Briefly, dibromomethane (10% in CH3CN) was fluorinated with K[18F]/K 2.2.2 in a glassy carbon reaction vessel at 120°?C for about 5?min to generate [18F]fluorobromomethane ([18F]FBM). The resulting [18F]FBM was then bubbling (He, 700?mL/min) through four Sep-Pak? Silica Plus Long cartridges to react with dimethylaminoethanol (10% DMAE in 0.3?mL DMSO) which was pre-loaded on Sep-Pak? C18 Plus Short cartridge. The [18F]FCH was purified by solid-phase extraction (SPE) using one Sep-Pak? C18 Plus Short and one Sep-Pak? CM Plus Short in series. The quality of [18F]FCH synthesized by this method was verified by HPLC and TLC as compared to authentic sample. Results Using this improved one-pot method, the RCY of [18F]FCH was 18.8 ± 2.1% (EOB, n = 27) in a synthesis time of 49 ± 5?min from EOB. The radiochemical purity of [18F]FCH was greater than 90% and the residual DMAE concentration in the final product was less than 10?ppm. Conclusions This optimized method could fulfill the demand of [18F]FCH for both pre-clinical and clinical studies, especially for nearby study sites without a cyclotron. ? 2017 Elsevier Ltd
SDGs
Other Subjects
Carbon; Diseases; Polyethylene terephthalates; Tumors; Dibromomethane; Hepatocellular carcinoma; One-pot synthesis; Prostate cancers; Radiochemical purity; Reaction vessel; Solid-phase extraction; [18F]FCH; Projectiles; deanol; dibromomethane; fluoromethylcholine f 18; tracer; unclassified drug; Article; controlled study; drug structure; drug synthesis; high performance liquid chromatography; one pot synthesis; priority journal; radiochemistry; solid phase extraction; thin layer chromatography
Type
journal article