[18F]Fluorination of o-carborane via nucleophilic substitution: towards a versatile platform for the preparation of 18F-labelled BNCT drug candidates

Kiran B. Gona; Vanessa Gómez-Vallejo; Daniel Padro; Jordi Llop

doi:10.1039/C3CC46695G

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[¹⁸F]Fluorination of o-carborane via nucleophilic substitution: towards a versatile platform for the preparation of ¹⁸F-labelled BNCT drug candidates†

Kiran B. Gona,^a Vanessa Gómez-Vallejo,^a Daniel Padro^b and Jordi Llop*^a

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* Corresponding authors

^a Radiochemistry Department, Molecular Imaging Unit, CIC biomaGUNE, Paseo Miramón 182, Parque Tecnológico de San Sebastian, San Sebastian, Spain
E-mail: jllop@cicbiomagune.es
Fax: +34 943 00 53 00
Tel: +34 943 00 53 33

^b Nuclear Magnetic Resonance Platform, CIC biomaGUNE, San Sebastian, Spain

Abstract

The mono-[¹⁸F]fluorination of o-carborane via nucleophilic substitution is reported. The new radiochemical transformation uses cyclotron produced [¹⁸F]F⁻ and a carboranyl iodonium salt. Further derivatization of the ¹⁸F-labelled carborane is achieved by formation of the C_c-lithio salt and reaction with an aldehyde.

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Article information

DOI: https://doi.org/10.1039/C3CC46695G
Article type: Communication
Submitted: 02 Sep 2013
Accepted: 11 Oct 2013
First published: 14 Oct 2013

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Chem. Commun., 2013,49, 11491-11493

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[¹⁸F]Fluorination of o-carborane via nucleophilic substitution: towards a versatile platform for the preparation of ¹⁸F-labelled BNCT drug candidates

K. B. Gona, V. Gómez-Vallejo, D. Padro and J. Llop, Chem. Commun., 2013, 49, 11491 DOI: 10.1039/C3CC46695G

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