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Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics

Lee, Chung-Cheng and Sui, Guodong and Elizarov, Arkadij and Shu, Chengyi Jenny and Shin, Young-Shik and Dooley, Alek N. and Huang, Jiang and Daridon, Antoine and Wyatt, Paul and Stout, David and Kolb, Hartmuth C. and Witte, Owen N. and Satyamurthy, Nagichettiar and Heath, James R. and Phelps, Michael E. and Quake, Stephen R. and Tseng, Hsian-Rong (2005) Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics. Science, 310 (5755). pp. 1793-1796. ISSN 0036-8075. doi:10.1126/science.1118919.

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Microreactor technology has shown potential for optimizing synthetic efficiency, particularly in preparing sensitive compounds. We achieved the synthesis of an [^(18)F]fluoride-radiolabeled molecular imaging probe, 2-deoxy-2-[18F]fluoro-d-glucose ([^(18)F]FDG), in an integrated microfluidic device. Five sequential processes—[^(18)F]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 [^(18)F]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.

Item Type:Article
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URLURL TypeDescription DOIArticle Online Material
Witte, Owen N.0000-0003-4461-4533
Heath, James R.0000-0001-5356-4385
Additional Information:© 2005 American Association for the Advancement of Science. 15 August 2005; accepted 15 November 2005. Supported by the U.S. Department of Energy–funded Institute for Molecular Medicine laboratory, the National Cancer Institute, the Norton Simon Research Foundation, the UCLA SOMI training program, NIH training grant 5T32-GM07616, and a collaboration between Molecular Imaging/Siemens and Fluidigm. We thank H. Padgett at Siemens for his contribution in radiochemical experiments.
Funding AgencyGrant Number
Department of Energy (DOE)UNSPECIFIED
Institute for Molecular Medicine LaboratoryUNSPECIFIED
National Cancer InstituteUNSPECIFIED
Norton Simon Research FoundationUNSPECIFIED
NIH Predoctoral Fellowship5T32-GM07616
Molecular ImagingUNSPECIFIED
Issue or Number:5755
Record Number:CaltechAUTHORS:20141119-084459417
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Official Citation:Lee, C.-C., Sui, G., Elizarov, A., Shu, C. J., Shin, Y.-S., Dooley, A. N., . . . Tseng, H.-R. (2005). Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics. Science, 310(5755), 1793-1796. doi: 10.1126/science.1118919
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:51937
Deposited On:19 Nov 2014 21:51
Last Modified:10 Nov 2021 19:18

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