A copper-catalyzed cycloamination of α-Csp3–H bond of N-aryl ketimines with sodium azide has been developed. This methodology provides an efficient access to quinoxalines and features mild reaction conditions and readily available ketimines with diverse functional group tolerance.

Copper(I)-catalyzed 5-sulfonation of quinolines via bidentate-chelation assistance has been developed. The reaction is compatible with a wide range of quinoline substrates and arylsulfonyl chlorides. Experimental and theoretical (DFT) investigation implicated that a single-electron-transfer process is involved in this sulfonylation transformation.

A carboamide-directed ruthenium-catalyzed C2-hydroindolation of alkynes has been described. This transformation provides a rapid access to free (N–H) C2-syn-alkenylated indole derivatives with the assistance of copper(II) salts, in which the directing group is removed via a one-pot process.