The first palladium-catalyzed highly regioselective indolization of 2-bromo- or 2-chloroanilines with internal alkynes: Synthesis of 2,3-disubstituted indoles

ORGN 391

Ming Shen, zlu@rdg.boehringer-ingelheim.com, Guisheng Li, Jianxiu Liu, Azad Hossain, Frank Roschangar, Vittorio Farina, Chris H. Senanayake, and Bruce Z. Lu, zlu@rdg.boehringer-ingelheim.com. Department of Chemical Development, Boehringer-Ingelheim Pharmaceuticals, Inc, 800 East Leigh Street, Suite 205, Richmond, VA 23219
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 chloro -anilines and their derivatives with internal alkynes.

 

Bioorganic, Metal-Mediated Reactions, and Molecular Recognition
8:00 PM-10:00 PM, Tuesday, 30 August 2005 Washington DC Convention Center -- Hall A, Poster

Division of Organic Chemistry

The 230th ACS National Meeting, in Washington, DC, Aug 28-Sept 1, 2005