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  • Title: Copper-Catalyzed Trifluoromethylation of Alkoxypyridine Derivatives.
    Author: Gyorfi N, Farkas E, Nemet N, Weber C, Novak Z, Kotschy A.
    Journal: Molecules; 2020 Oct 16; 25(20):. PubMed ID: 33081411.
    Abstract:
    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.
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