Synthetic Route to Chiral Tetrahydroquinoxalines via Ring-Opening of Activated Aziridines

A highly regio- and stereoselective route for the synthesis of racemic and nonracemic tetrahydroquinoxalines via the S_N2-type ring-opening of activated aziridines with 2-bromoanilines followed by the Pd-catalyzed intramolecular C–N bond formation is described.