1 Department of Chemical Development, Boehringer-Ingelheim Pharmaceuticals, Inc., Suite 205, East Leigh Street, Richmond, Virginia 23219, USA. [email protected]
[Structure: see text] A practical one-pot, regiospecific three-component process for the synthesis of 2,3-disubstituted indoles was developed via consecutive Pd-catalyzed Sonogashira coupling, amidopalladation, and reductive elimination.