Enhanced copper-mediated 18F-fluorination of aryl boronic esters provides eight 
radiotracers for PET applications

Preshlock, Sean; Calderwood, Samuel; Verhoog, Stefan; Tredwell, Mathew; Huiban, Mickael; Hienzsch, Antje; Gruber, Stefan; Wilson, Thomas C.; Taylor, Nicholas J.; Caily, Thomas; Schedler, Michael; Colier, Thomas Lee; Passchier, Jan; Smits, René; Molitor, Jan; Hoepping, Alexander; Mueller, Marco; Genicot, Christoph; Mercier, Joel; gouverneur, Véronique

doi:10.1039/C6CC03295H

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Enhanced copper-mediated ¹⁸F-fluorination of aryl boronic esters provides eight radiotracers for PET applications

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Tredwell, Mathew
Research Group Tredwell, Max-Planck-Institut für Kohlenforschung, Max Planck Society;

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Citation

Preshlock, S., Calderwood, S., Verhoog, S., Tredwell, M., Huiban, M., Hienzsch, A., et al. (2016). Enhanced copper-mediated ¹⁸F-fluorination of aryl boronic esters provides eight radiotracers for PET applications. Chemical Communications, 52, 8361-8364. doi:10.1039/C6CC03295H.

Cite as: https://hdl.handle.net/11858/00-001M-0000-002D-B122-5

Abstract

[¹⁸F]FMTEB, [¹⁸F]FPEB, [¹⁸F]flumazenil, [¹⁸F]DAA1106, [¹⁸F]MFBG, [¹⁸F]FDOPA, [¹⁸F]FMT and [¹⁸F]FDA are prepared from the corresponding arylboronic esters and [¹⁸F]KF/K222 in the presence of Cu(OTf)₂py₄. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of ¹⁸F-fluoride.