Synthesis of Axially Chiral Olefin–Oxazoline Ligands via Pd-Catalyzed Multiple C–H Functionalization

We report herein the Pd-catalyzed oxazoline-directed C–H olefination of the N-arylindole skeleton, affording two diastereomers of axially chiral olefin–oxazoline ligands in a one-step procedure. Modifications at the 3- and 3′-positions were facilely achieved via electrophilic substitution of the indole fragment and subsequent oxazoline-directed C–H amidation or olefination of the arene fragment.