Issue 53, 2024

Synthesis of 18F-labelled aryl trifluoromethyl ketones with improved molar activity

Abstract

A method for the radiosynthesis of 18F-labelled aryl trifluoromethyl ketones starting from widely available Weinreb amides using [18F]fluoroform is presented. The method uses potassium hexamethyldisilazane as base and delivers products in high molar activity (up to 24 GBq μmol−1) and excellent radiochemical conversions. The applicability for PET tracer synthesis is demonstrated by the radiosynthesis of ten (hetero)aryl trifluoromethylketones, bearing electron-withdrawing and -donating substituents including a derivative of bioactive probenecid.

Graphical abstract: Synthesis of 18F-labelled aryl trifluoromethyl ketones with improved molar activity

Supplementary files

Article information

Article type
Communication
Submitted
15 Apr 2024
Accepted
07 Jun 2024
First published
10 Jun 2024
This article is Open Access
Creative Commons BY-NC license

Chem. Commun., 2024,60, 6801-6804

Synthesis of 18F-labelled aryl trifluoromethyl ketones with improved molar activity

L. Veth, A. D. Windhorst and D. J. Vugts, Chem. Commun., 2024, 60, 6801 DOI: 10.1039/D4CC01776E

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. You can use material from this article in other publications, without requesting further permission from the RSC, provided that the correct acknowledgement is given and it is not used for commercial purposes.

To request permission to reproduce material from this article in a commercial publication, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party commercial publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements