Exceedingly Fast Copper(II)-Promoted ortho C–H Trifluoromethylation of Arenes using TMSCF3
Ming Shang, Shang-Zheng Sun, Hong-Li Wang, Brian N. Laforteza, Hui-Xiong Dai and Jin-Quan Yu
Angew. Chem. Int. Ed.,
2014, 39, 10439-10442; 10.1002/anie.201404822
08/2014
The Yu Group disclose the direct ortho-trifluoromethylation of arenes and heteroarenes using TMSCF3.
Using a copper(II)-catalyzed C–H functionalization this pharmaceutically significant functional group can be introduced in under 30 minutes to a broad range of substrates. Mechanistic studies confirm the involvement of C–H activation rather than electrophilic aromatic substitution.