Selective Copper-Promoted Cross-Coupling of Aromatic Amines with Alkyl Boronic Acids

Abstract

A simple copper-promoted N-monoalkylation of anilines that utilizes alkyl boronic acids as the alkylating partner is presented. The reaction is carried out in refluxing dioxane, and it 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.

alkylation - copper - cross-coupling - boron - amines

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