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Petasis Boronic Mannich Reactions of Electron-Poor Aromatic Amines under Microwave Conditions

Markus Follmann*, Franziska Graul, Thorsten Schäfer, Sebastian Kopec, Peter Hamley

*Aventis Pharma Deutschland GmbH, a company of the sanofi-aventis group, Industriepark Höchst, G838, 65926 Frankfurt am Main, Germany, Email:

M. Follmann, F. Gaul, T Schäfer, S. Kopec, P. Hamley, Synlett, 2005, 1009-1011.

DOI: 10.1055/s-2005-864817


The Petasis reaction of electron-poor aromatic amines such as aminopyridines under microwave irradiation provides rapid access to a number of unnatural N-aryl-α-amino acids. The influence of the electronic demand of the boronic acids on the yields is discussed. A comparison with conventional heating is provided.

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Key Words

Petasis Reaction, amino acids, boron, green chemistry, heterocycles, multicomponent reactions, microwave synthesis

ID: J60-Y2005-030