Copper-Catalyzed Formamidation of Arylboronic Acids: Direct Access to Formanilides

Abstract

A new approach for direct synthesis of formanilides starting from structurally varied arylboronic acids is reported. The protocol involves a copper-catalyzed Chan–Lam coupling reaction between arylboronic acids and formamide in the presence of a base at room temperature. The strategy offers a valid and practical alternative to existing transformations of amino, nitro, and azido arenes to formanilides, especially in terms of executing arylboronic acids as easily accessible, stable, and diversified substrates, under mild reaction conditions, and in a simple operation with high efficiency.

Key words

formamide - formanilides - arylboronic acids - C–N cross-coupling - N-arylation

• References and Notes

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