The First Regioselective Palladium-Catalyzed Indolization of 2-Bromo- or 2-Chloroanilines with Internal Alkynes: A New Approach to 2,3-Disubstituted Indoles

The first practical and economical process for synthesis of 2,3-disubstituted indole compounds has been developed with high regioselectivity by palladium-catalyzed indolization of 2-bromo- or chloroanilines and their derivatives with internal alkynes.