Iridium(III)-Catalyzed Regioselective C7-Amination of <i>N</i>-Pivaloylindoles with Sulfonoazides

Abstract

Direct C7-amination of N -pivaloylindoles has been achieved using a combination of [Cp*IrCl 2 ] 2, AgNTf 2, and AgOAc as the catalyst and sulfonoazides as the nitrogen source. The reaction proceeded at room temperature to 80 °C to afford 7-sulfonamidoindoles in good to excellent yields. The reaction is broadly applicable to the C7-amination of a wide variety of 3-, 4-, 5-, and 6-substituted N -pivaloylindoles with either alkyl or aryl sulfonoazides.