Copper‐mediated Intermolecular C−H aminohalogenation of Indoles at Room Temperature

Abstract

An efficient intermolecular CÀ H aminohalogenation of indoles with azoles and NXS (X = F, Cl, Br, I) has been developed. This mild protocol provides a straightforward entry to structurally valuable 2-azolyl-3-halogenated indoles in one single operation. In addition, this attractive route for the synthesis of polyfunctionalized indoles is of great significance due to the product's versatile reactivity for further transformations.

Iron–iodine co-catalysis towards tandem C–N/C–C bond formation: one-pot regioselective synthesis of 2-amino-3-alkylindoles

“…Therefore, as part of our ongoing efforts toward the development of methodologies for the preparation and functionalization of indoles, 16 we recently reported an efficient copper–iodine co-catalyzed 2,3-difunctionalization of indoles with azoles and phenols via temperature-controlled selectivity switch for the efficient synthesis of 2-azolyl-3-alkenylindoles. 16 e Nevertheless, the development of intermolecular aminoalkylation of carbon–carbon double bonds of indoles remains unexplored.…”