Copper‐Catalyzed Coupling Reaction of Diazo Reagent with Formamide for the Synthesis of α‐Formyloxy Ketones and α‐Ketoamides

A copper‐catalyzed coupling reaction of diazo reagents with formamides is reported. Under the optimal reaction conditions, this reaction leads to a wide range of α‐formyloxy ketones and α‐ketoamides in moderate to good yields. This strategy enables the installation of two important functional groups, aldehyde and amine group, into the target molecule in the presence of formamide via CN bond cleavage. Mechanism studies indicate that this conversion reaction may undergo a radical process.