Minimalist approach meets green chemistry: Synthesis of F- labeled (hetero)aromatics in pure ethanol.

Boris D Zlatopolskiy, Johannes Zischler, Philipp Krapf, Raphael Richarz, Katharina Lauchner, Bernd Neumaier

Journal: Journal of labelled compounds & radiopharmaceuticals 2020;62(8):404-410

PMID: 31162691

Abstract

The application of toxic solvents and additives is inevitable for most of the described protocols for F-labeling. Herein, a novel "green" procedure for nucleophilic aromatic radiofluorination of highly activated (hetero)aromatic substrates in pure EtOH is described. Using this method a series of F-labeled (hetero)arenes have been synthesized in radiochemical yields (RCYs) of up to 97%.

Address: Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, Jülich, Germany.; Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Cologne, Germany.; Max Planck Institute for Metabolism Research, Cologne, Germany.

DOI: 10.1002/jlcr.3776

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https://doi.org/10.1002/jlcr.3776

MeSH Terms: Chemistry Techniques, Synthetic, Ethanol, Fluorine Radioisotopes, Green Chemistry Technology, Isotope Labeling, Radiochemistry