Ascertaining the suitability of aryl sulfonyl fluorides for [18F]radiochemistry applications: a systematic investigation using microfluidics
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Date
2013-10-18
Journal Title
Journal ISSN
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Publisher
American Chemical Society
Abstract
Optimization of [18F]radiolabeling conditions and subsequent stability analysis in mobile phase, PBS buffer, and rat serum of 12 aryl sulfonyl chloride precursors with various substituents (electron-withdrawing groups, electron-donating groups, increased steric bulk, heterocyclic) were performed using an Advion NanoTek Microfluidic Synthesis System. A comparison of radiochemical yields and reaction times for a microfluidics device versus a conventional reaction vessel is reported. [18F]Radiolabeling of sulfonyl chlorides in the presence of competing nucleophiles, H-bond donors, and water was also assessed and demonstrated the versatility and potential utility of [18F]sulfonyl fluorides as synthons for indirect radiolabeling. © 2013 American Chemical Society
Description
Keywords
Positron computed tomography, Radiopharmaceuticals, Labelled compounds, Fluids, Radiochemistry, Molecules
Citation
Matesic, L., Wyatt, N. A., Fraser, B. H., Roberts, M. P., Pham, T. Q., & Greguric, I. (2013). Ascertaining the suitability of aryl sulfonyl fluorides for [18F] radiochemistry applications: a systematic investigation using microfluidics. The Journal of Organic Chemistry, 78(22), 11262-11270. doi:10.1021/jo401759z