Boron-catalyzed α-C–H fluorination of aryl acetic acids

Abstract

The catalytic α-C–H fluorination of aryl acetic acids was achieved with good functional group tolerance in the presence of a boron catalyst. A series of α-fluoro aryl acetic acids were obtained in a single step with high yields (up to 96%). The catalytic reaction was employed for the synthesis of bioactive molecules and the modification of profen drugs. Moreover, the reaction could be performed on a gram scale. Further transformations were carried out.