A Universal Procedure for the [F-18]Trifluoromethylation of Aryl Iodides and Aryl Boronic Acids with Highly Improved Specific Activity

Autor: Albert D. Windhorst, Dion van der Born, Romano V. A. Orru, Claudia Sewing, J. Koos D. M. Herscheid, Danielle J. Vugts
Přispěvatelé: Organic Chemistry, AIMMS, Neuroscience Campus Amsterdam - Brain Imaging Technology, Radiology and nuclear medicine, CCA - Disease profiling, NCA - Brain imaging technology
Jazyk: angličtina
Rok vydání: 2014
Předmět:
Zdroj: van der Born, D, Sewing, C, Herscheid, J D M, Windhorst, A D, Orru, R V A & Vugts, D J 2014, ' A Universal Procedure for the [F-18]Trifluoromethylation of Aryl Iodides and Aryl Boronic Acids with Highly Improved Specific Activity ', Angewandte Chemie International Edition in English, vol. 53, no. 41, pp. 11046-11050 . https://doi.org/10.1002/anie.201406221
Angewandte Chemie International Edition in English, 53(41), 11046-11050. John Wiley and Sons Ltd
ISSN: 0570-0833
1433-7851
DOI: 10.1002/anie.201406221
Popis: Herein, we describe a valuable method for the introduction of the [(18)F]CF3 group into arenes with highly improved specific activity by the reaction of [(18)F]trifluoromethane with aryl iodides or aryl boronic acids. This [(18)F]trifluoromethylation reaction is the first to be described in which the [(18)F]CF3 products are generated in actual trace amounts and can therefore effectively be used as PET tracers. The method shows broad scope with respect to possible aryl iodide and aryl boronic acid substrates, as well as good to excellent conversion. In particular, the [(18)F]trifluoromethylation of boronic acids was found to outperform [(18)F]trifluoromethylation reactions of halogenated aryl precursors with regard to conversion, reaction conditions, and kinetics.
Databáze: OpenAIRE
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