Selective Copper-Promoted Cross-Coupling of Aromatic Amines with Alkyl Boronic Acids
Marta Larrosa, César Guerrero, Ramón Rodríguez, Jacobo Cruces*
*GalChimia, S.L., R&D Department, Cebreiro s/n, 15823 O Pino, A Coruña, Spain, Email: jacobo.crucesgalchimia.com
M. Larrosa, C. Guerrero, R. Rodríguez, J. Cruces, Synlett, 2010, 2101-2105.
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A simple copper-promoted N-monoalkylation of anilines that utilizes alkyl boronic acids as the alkylating partner is carried out in refluxing dioxane and allows a number of structurally and electronically diverse anilines to be functionalized in a single step. A broad study was carried out to demonstrate the utility of this new methodology for the preparation of phenethylanilines.
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I. González, J. Mosquera, C. Guerrero, R. Rodríguez, Jacobo Cruces, Org. Lett., 2009, 11, 1677-1680.