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Synthesis of aromatic trifluoromethyl compounds: The potential for large scale application


Solvias AG, Römerpark 2, 4303 Kaiseraugst, Switzerland


This article provides an overview on reagents and protocols for the synthesis of aromatic trifluoromethyl compounds. The generation of trifluoromethylated aromatic building blocks, the deoxoflurination of carboxylic acids, and the trifluoromethylation of aromatic precursors are covered by this review. Issues that favor or hinder the large scale application of particular reagents and protocols are presented. Remarkably, only one out of more than 10 protocols covered by this review is currently applied on large production scale, a few others have been applied on a 5 kg to 100 kg scale.



Trifluoromethylated aromatic rings are common motifs in pharmaceutical and agrochemical active compounds as well as in performance materials (1). For many decades, formation of aryl-CF3 compounds has been limited to a few traditional technologies, espe ... ...

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