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18F-Labeling of Aryl-SCF3, -OCF3and -OCHF2with [18F]Fluoride

Khotavivattana, Tanatorn, Verhoog, Stefan, Tredwell, Matthew, Pfeifer, Lukas, Calderwood, Samuel, Wheelhouse, Katherine, Collier, Thomas Lee and Gouverneur, Veronique 2015. 18F-Labeling of Aryl-SCF3, -OCF3and -OCHF2with [18F]Fluoride. Angewandte Chemie International Edition 54 (34) , pp. 9991-9995. 10.1002/anie.201504665

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Abstract

We report that halogenophilic silver(I) triflate permits halogen exchange (halex) nucleophilic 18F‐fluorination of aryl‐OCHFCl, ‐OCF2Br and ‐SCF2Br precursors under mild conditions. This AgI‐mediated process allows for the first time access to a range of 18F‐labeled aryl‐OCHF2, ‐OCF3 and ‐SCF3 derivatives, inclusive of [18F]riluzole. The 18F‐labeling of these medicinally important motifs expands the radiochemical space available for PET applications.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Medicine
Publisher: Wiley
ISSN: 1433-7851
Last Modified: 12 Jun 2019 10:59
URI: http://orca.cf.ac.uk/id/eprint/122210

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