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A Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones

Marc Nazaré*, Claudia Schneider, Andreas Lindenschmidt, David William Will

*Aventis Pharma Deutschland GmbH, Medicinal Chemistry, DI&A Chemistry, Building G878, 65926 Frankfurt am Main, Germany, Email:

M. Nazare, C. Schneider, A. Lindenschmidt, D. W. Will, Angew. Chem. Int. Ed., 2004, 43, 4526-4528.

DOI: 10.1002/anie.200460122 (free Supporting Information)


A new, mild, and efficient method for the synthesis of polyfunctionalized indoles by direct reaction of substituted 2-chloroanilines with cyclic or acyclic ketones was developed. This procedure is simple to carry out and broadly applicable.

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Key Words

annulation, cyclization, indoles, azaindoles, nitrogen heterocycles, palladium

ID: J06-Y2004-530