Cross-coupling of [11C]methyllithium for 11C-labelled PET tracer synthesis

Hugo Helbert; Ines Farinha Antunes; Gert Luurtsema; Wiktor Szymanski; Ben L. Feringa; Philip H. Elsinga

doi:10.1039/D0CC05392A

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Cross-coupling of [¹¹C]methyllithium for ¹¹C-labelled PET tracer synthesis†

Hugo Helbert,^ab Ines Farinha Antunes,^b Gert Luurtsema,^b Wiktor Szymanski,

^c Ben L. Feringa

*^a and Philip H. Elsinga*^b

Author affiliations

* Corresponding authors

^a Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 4, Groningen, The Netherlands
E-mail: b.l.feringa@rug.nl

^b Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands
E-mail: p.h.elsinga@umcg.nl

^c Department of Radiology, University of Groningen, University Medical Center Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands

Abstract

The cross-coupling of aryl bromides with [¹¹C]CH₃Li for the labelling of a variety of tracers for positron emission tomography (PET) is presented. The radiolabelled products were obtained in excellent yields, at rt and after short reaction times (3–5 min) compatible with the half-life of ¹¹C (20.4 min). The automation of the protocol on a synthesis module is investigated, representing an important step towards a fast method for the synthesis of ¹¹C-labelled compounds for PET imaging.

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Article information

DOI: https://doi.org/10.1039/D0CC05392A
Article type: Communication
Submitted: 07 Aug 2020
Accepted: 26 Nov 2020
First published: 26 Nov 2020

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Chem. Commun., 2021,57, 203-206

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Cross-coupling of [¹¹C]methyllithium for ¹¹C-labelled PET tracer synthesis

H. Helbert, I. F. Antunes, G. Luurtsema, W. Szymanski, B. L. Feringa and P. H. Elsinga, Chem. Commun., 2021, 57, 203 DOI: 10.1039/D0CC05392A

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