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Open AccessArticle

Copper-Catalyzed Trifluoromethylation of Alkoxypyridine Derivatives

Servier Research Institute of Medicinal Chemistry, Záhony u. 7., H-1031 Budapest, Hungary
Institute of Chemistry, Eötvös Loránd Unversity, Pázmány Péter s. 1/A, H-1117 Budapest, Hungary
Author to whom correspondence should be addressed.
Academic Editors: Ferenc Fulop and Dariusz Matosiuk
Molecules 2020, 25(20), 4766;
Received: 18 September 2020 / Revised: 9 October 2020 / Accepted: 13 October 2020 / Published: 16 October 2020
The trifluoromethylation of aromatic and heteroaromatic cores has attracted considerable interest in recent years due to its pharmacological relevance. We studied the extension of a simple copper-catalyzed trifluoromethylation protocol to alkoxy-substituted iodopyridines and their benzologs. The trifluoromethylation proceeded smoothly in all cases, and the desired compounds were isolated and characterized. In the trifluoromethylation of 3-iodo-4-methoxyquinoline, we observed a concomitant O-N methyl migration, resulting in the trifluoromethylated quinolone as a product. Overall, the described procedure should facilitate the broader use of copper-catalyzed trifluoromethylation in medicinal chemistry. View Full-Text
Keywords: trifluoromethylation; copper catalysis; heterocycles trifluoromethylation; copper catalysis; heterocycles
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MDPI and ACS Style

Gyorfi, N.; Farkas, E.; Nemet, N.; Weber, C.; Novak, Z.; Kotschy, A. Copper-Catalyzed Trifluoromethylation of Alkoxypyridine Derivatives. Molecules 2020, 25, 4766.

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