Mild and Soft Catalyzed Trifluoromethylthiolation of Boronic Acids: The Crucial Role of Water

Chemistry. 2015 Oct 12;21(42):14694-8. doi: 10.1002/chem.201502338. Epub 2015 Aug 13.

Abstract

The most reactive 2nd generation of trifluoromethanesulfenamides undergoes a copper-catalyzed cross-coupling reaction with boronic acids to afford CF3 S-molecules. Contrary to the previous methods in the literature, no base addition, no heating, and no large excess of reagents are required to obtain good results. Furthermore, a crucial role of a small amount of water to favor this reaction has been demonstrated. This constitutes the mildest described conditions for such a reaction.

Keywords: boronic acid; cross-coupling; fluorine; trifluoromethanesulfenamide; trifluoromethylthiolation.