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The first regioselective palladium-catalyzed indolization of 2-bromo- or 2-chloroanilines with internal alkynes: a new approach to 2,3-disubstituted indoles
Authors:Shen Ming  Li Guisheng  Lu Bruce Z  Hossain Azad  Roschangar Frank  Farina Vittorio  Senanayake Chris H
Institution:Department of Chemical Development, Boehringer-Ingelheim Pharmaceuticals, Inc., 800 East Leigh Street, Suite 205, Richmond, Virginia 23219, USA.
Abstract:reaction: see text] 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.
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