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

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.

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Item Permalink: https://hdl.handle.net/11858/00-001M-0000-002D-B122-5 Version Permalink: https://hdl.handle.net/11858/00-001M-0000-002D-B123-3

Genre: Journal Article

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Creators:
Preshlock, Sean¹, Author
Calderwood, Samuel¹, Author
Verhoog, Stefan¹, Author
Tredwell, Mathew², Author
Huiban, Mickael³, Author
Hienzsch, Antje⁴, Author
Gruber, Stefan¹, Author
Wilson, Thomas C.¹, Author
Taylor, Nicholas J.¹, Author
Caily, Thomas^{1, 5}, Author
Schedler, Michael¹, Author
Colier, Thomas Lee⁶, Author
Passchier, Jan³, Author
Smits, René⁴, Author
Molitor, Jan⁴, Author
Hoepping, Alexander⁴, Author
Mueller, Marco⁴, Author
Genicot, Christoph⁷, Author
Mercier, Joel⁷, Author
gouverneur, Véronique¹, Author

Affiliations:
1University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK , ou_persistent22
2Research Group Tredwell, Max-Planck-Institut für Kohlenforschung, Max Planck Society, Kaiser-Wilhelm-Platz 1, 45470 Mülheim an der Ruhr, DE, ou_2466692
3Imanova, Burlington Danes building Imperial College, London Hammersmith Hospital, Du Cane Road, London W12 0NN, UK, ou_persistent22
4ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany, ou_persistent22
5Normandie University, UNICAEN, CERMN, F-14032 Caen, France , ou_persistent22
6Advion BioSystems, 10 Brown Road, Suite 101, Ithaca, USA, ou_persistent22
7Global Chemistry, UCB New Medicines, UCB Biopharma sprl, 1420 Braine-L'Alleud, Belgium, ou_persistent22

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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.

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Language(s): eng - English

Dates: Accepted: 2016-05-23Published Online: 2016-05-23Date issued: 2016-07-11

Publication Status: Issued

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Rev. Type: Peer

Identifiers: DOI: 10.1039/C6CC03295H

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Title: Chemical Communications

Abbreviation : Chem. Commun.

Source Genre: Journal

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Publ. Info: Cambridge, UK : Royal Society of Chemistry

Pages: - Volume / Issue: 52 Sequence Number: - Start / End Page: 8361 - 8364 Identifier: ISSN: 1359-7345
CoNE: https://pure.mpg.de/cone/journals/resource/954928495413