Minimalist approach meets green chemistry: Synthesis of 18 F- labeled (hetero)aromatics in pure ethanol

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

doi:10.1002/jlcr.3776

Minimalist approach meets green chemistry: Synthesis of ¹⁸ F- labeled (hetero)aromatics in pure ethanol

J Labelled Comp Radiopharm. 2019 Jun 30;62(8):404-410. doi: 10.1002/jlcr.3776.

Authors

Boris D Zlatopolskiy^{1

2

3}, Johannes Zischler^{1

2}, Philipp Krapf^{1

2}, Raphael Richarz^{1

2}, Katharina Lauchner^{1

2}, Bernd Neumaier^{1

2

3}

Affiliations

¹ Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, Jülich, Germany.
² Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Cologne, Germany.
³ Max Planck Institute for Metabolism Research, Cologne, Germany.

PMID: 31162691
DOI: 10.1002/jlcr.3776

Abstract

The application of toxic solvents and additives is inevitable for most of the described protocols for ¹⁸ 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 ¹⁸ F-labeled (hetero)arenes have been synthesized in radiochemical yields (RCYs) of up to 97%.

Keywords: (hetero)aromatics; PSMA; green chemistry; minimalist approach; radiofluorination; sustainability.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Chemistry Techniques, Synthetic
Ethanol / chemical synthesis*
Ethanol / chemistry*
Fluorine Radioisotopes / chemistry*
Green Chemistry Technology
Isotope Labeling
Radiochemistry

Substances

Fluorine Radioisotopes
Ethanol
Fluorine-18

Abstract

Publication types

MeSH terms

Substances

Grants and funding