Copper-Mediated Bis(trifluoromethyl)carbinolation of Arylboronic Acids Enabled by Iodobis(trifluoromethyl)carbinol Ester

The bis(trifluoromethyl)carbinol motif represents a privileged pharmacophore, yet its efficient construction, especially at a late stage, remains an unmet challenge. Here, we introduce iodobis(trifluoromethyl)carbinol ester (I-BTFCE) as a stable solid reagent that enables the hitherto Cu(I)-mediated bis(trifluoromethyl)carbinolation of arylboronic acids. This method provides streamlined access to diverse aryl bis(trifluoromethyl)carbinols, including natural product and pharmaceutical derivatives. The discovery of potent antiproliferative activity among the synthesized products highlights the significant biological potential of this synthetic method.