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Direct Palladium-Catalyzed C-3 Arylation of Free (NH)-Indoles with Aryl Bromides under Ligandless Conditions

Fabio Bellina, Francesca Benelli and Renzo Rossi*

*Dipartimento di Chimica e Chimica Industriale, University of Pisa, Via Risorgimento 35, 56125 Pisa, Italy, Email:

F. Bellina, F. Benelli, R. Rossi, J. Org. Chem., 2008, 73, 5529-5535.

DOI: 10.1021/jo8007572


An efficient, practical, and highly regioselective direct palladium-catalyzed C-3 arylation of electron-rich free (NH)-indoles with various aryl bromides under ligandless conditions in refluxing toluene in the presence of K2CO3 as the base can be run outside a glovebox without purification of solvent and reagents.

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Key Words

Indoles, Arylation

ID: J42-Y2008-1880