An Axially Chiral Styrene-Phosphine Ligand for Pd-Catalyzed Asymmetric N -Alkylation of Indoles.

An efficient palladium-catalyzed enantioselective direct N -alkylation of indoles using a novel type of axially chiral styrene-phosphine ligand SJTU-PHOS-1 was developed. This reaction demonstrated good functional group compatibility and a wide range scope of substrates in mild conditions. Moreover, the DFT calculations expounded the coordination mode of the metal catalyst and the axially chiral styrene-phosphine ligand in the enantioselectivity control.