Au(III)/TPPMS-catalyzed Friedel-Crafts benzylation of deactivated N -alkylanilines in water.

The Friedel-Crafts reaction of electronically deactivated anilines including those with strong electron-withdrawing NO 2 , CN or CO 2 H groups is challenging due to the reduced electron density of the aromatic ring. Here, we demonstrate the Au(III)/TPPMS-catalyzed Friedel-Crafts benzylation of deactivated anilines in water. This reaction exhibits operational simplicity and a broad substrate scope with high regioselectivity, enabling rapid access to 2-benzylanilines.