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Updated: Jun 24, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Synthesis of 18F-labelled aryl trifluoromethyl ketones with improved molar activity
Lukas Veth1, Albert D Windhorst1, Danielle J Vugts1
1Dept. of Radiology & Nuclear Medicine Amsterdam UMC, Location Vrije Universiteit Amsterdam De Boelelaan, 1117, Amsterdam, The Netherlands. l.r.veth@amsterdamumc.nl.
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.
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