Trisoxazoline/Cu(II)-catalyzed asymmetric intramolecular Friedel-Crafts alkylation reaction of indoles

Intramolecular Friedel-Crafts alkylation reaction of indoles catalyzed by trisoxazoline/copper(II) is described. This annulation provides an easy access to polycyclic indole derivatives with up to 90% ee in up to 99% yield.

An intramolecular Friedel-Crafts alkylation reaction of indoles has been developed and up to 90% ee is achieved in high to excellent yields by empolying trisoxazoline/copper(II) as a catalyst.