[18F]fluoro-benziodoxole: a no-carrier-added electrophilic fluorinating reagent. Rapid, simple radiosynthesis, purification and application for fluorine-18 labelling

Miguel A. Cortés González; Patrik Nordeman; Antonio Bermejo Gómez; Denise N. Meyer; Gunnar Antoni; Magnus Schou; Kálmán J. Szabó

doi:10.1039/C8CC00526E

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[¹⁸F]fluoro-benziodoxole: a no-carrier-added electrophilic fluorinating reagent. Rapid, simple radiosynthesis, purification and application for fluorine-18 labelling†

Miguel A. Cortés González,

^a Patrik Nordeman,^b Antonio Bermejo Gómez,

^ac Denise N. Meyer,

^a Gunnar Antoni,^b Magnus Schou^c and Kálmán J. Szabó

*^a

Author affiliations

* Corresponding authors

^a Department of Organic Chemistry, Stockholm University, Sweden
E-mail: kalman.j.szabo@su.se
Web: http://www.organ.su.se/ks/

^b Department of Medicinal Chemistry, Uppsala University, Sweden

^c AstraZeneca PET Centre at Karolinska Institutet, Stockholm, Sweden

Abstract

Operationally simple radiosynthesis and purification of [¹⁸F]fluoro-benziodoxole was developed starting from a cyclotron produced [¹⁸F]F⁻ precursor, [¹⁸F]TBAF, and tosyl-benziodoxole. The synthetic utility of [¹⁸F]fluoro-benziodoxole was demonstrated by electrophilic fluorocyclization of o-styrilamides proceeding with high RCC (typically 50–90%) and high molar activity (up to 396 GBq μmol⁻¹).

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Article information

DOI: https://doi.org/10.1039/C8CC00526E
Article type: Communication
Submitted: 22 Jan 2018
Accepted: 03 Apr 2018
First published: 03 Apr 2018
This article is Open Access

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Chem. Commun., 2018,54, 4286-4289

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[¹⁸F]fluoro-benziodoxole: a no-carrier-added electrophilic fluorinating reagent. Rapid, simple radiosynthesis, purification and application for fluorine-18 labelling

M. A. Cortés González, P. Nordeman, A. Bermejo Gómez, D. N. Meyer, G. Antoni, M. Schou and K. J. Szabó, Chem. Commun., 2018, 54, 4286 DOI: 10.1039/C8CC00526E

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