Issue 68, 2021

Base-catalysed 18F-labelling of trifluoromethyl ketones. Application to the synthesis of 18F-labelled neutrophil elastase inhibitors

Abstract

A new method for the fluorine-18 labelling of trifluoromethyl ketones has been developed. This method is based on the conversion of a–COCF3 functional group to a difluoro enol silyl ether followed by halogenation and fluorine-18 labelling. The utility of this new method was demonstrated by the synthesis of fluorine-18 labelled neutrophil elastase inhibitors, which are potentially useful for detection of inflammatory disorders.

Graphical abstract: Base-catalysed 18F-labelling of trifluoromethyl ketones. Application to the synthesis of 18F-labelled neutrophil elastase inhibitors

Supplementary files

Article information

Article type
Communication
Submitted
06 Jul 2021
Accepted
30 Jul 2021
First published
30 Jul 2021
This article is Open Access
Creative Commons BY-NC license

Chem. Commun., 2021,57, 8476-8479

Base-catalysed 18F-labelling of trifluoromethyl ketones. Application to the synthesis of 18F-labelled neutrophil elastase inhibitors

D. N. Meyer, M. A. Cortés González, X. Jiang, L. Johansson-Holm, M. Pourghasemi Lati, M. Elgland, P. Nordeman, G. Antoni and K. J. Szabó, Chem. Commun., 2021, 57, 8476 DOI: 10.1039/D1CC03624F

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