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

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 radio...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2024-06, Vol.60 (53), p.6801-6804
Main Authors: Veth, Lukas, Windhorst, Albert D, Vugts, Danielle J
Format: Article
Language:English
Subjects:
Amides
Aromatic compounds
Ketones
Radiochemistry
Synthesis
Trifluoromethane
Online Access:Get full text
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Summary: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.
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/d4cc01776e