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Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics
- Lee, Chung-Cheng, Sui, Guodong, Elizarov, Arkadij, Shu, Chengyi Jenny, Shin, Young-Shik, Dooley, Alek N., Huang, Jiang, Daridon, Antoine, Wyatt, Paul, Stout, David, Kolb, Hartmuth C., Witte, Owen N., Satyamurthy, Nagichettiar, Heath, James R., Phelps, Michael E., Quake, Stephen R., Tseng, Hsian-Rong
- Science 2005 v.310 no.5755 pp. 1793-1796
- evaporation, fluorides, image analysis, mice, positron-emission tomography, radiolabeling, solvents
- Microreactor technology has shown potential for optimizing synthetic efficiency, particularly in preparing sensitive compounds. We achieved the synthesis of an [¹⁸F]fluoride-radiolabeled molecular imaging probe, 2-deoxy-2-[¹⁸F]fluoro-D-glucose ([¹⁸F]FDG), in an integrated microfluidic device. Five sequential processes--[¹⁸F]fluoride concentration, water evaporation, radiofluorination, solvent exchange, and hydrolytic deprotection--proceeded with high radio-chemical yield and purity and with shorter synthesis time relative to conventional automated synthesis. Multiple doses of [¹⁸F]FDG for positron emission tomography imaging studies in mice were prepared. These results, which constitute a proof of principle for automated multistep syntheses at the nanogram to microgram scale, could be generalized to a range of radiolabeled substrates.