A Fluorinated Ligand Enables Room-Temperature and Regioselective Pd-Catalyzed Fluorination of Aryl Triflates and Bromides

作者：Sather Aaron C; Lee Hong Geun; De la Rosa Valentina Y; Yang Yang; Mueller Peter; Buchwald Stephen L^*

来源：Journal of the American Chemical Society, 2015, 137(41): 13433-13438.

DOI：10.1021/jacs.5b09308

A new biaryl monophosphine ligand (AlPhos, L1) allows for the room-temperature Pd-catalyzed fluorination of a variety of activated (hetero)aryl trifiates. Furthermore, aryl triflates and bromides that are prone to give mixtures of regioisomeric aryl fluorides with Pd-catalysis can now be converted to the desired aryl fluorides with high regioselectivity. Analysis of the solid-state structures of several Pd(II) complexes, as well as density functional theory (DFT) calculations, shed light on the origin of the enhanced reactivity observed with L1.

• 出版日期2015-10-21