Regioselective Chlorination of Quinoline <i>N</i>‐Oxides and Isoquinoline <i>N</i>‐Oxides Using PPh₃/Cl₃CCN

Abstract

Abstract A novel method for the regioselective C2‐chlorination of heterocyclic N ‐oxides has been developed. PPh 3 /Cl 3 CCN were used as chlorinating reagents and the desired N‐heterocyclic chlorides were obtained smoothly in satisfactory yields. The reactions proceeded in a highly efficient and selective manner across a broad range of substrates demonstrating excellent functional group tolerance. In addition, this chlorination reaction can be used for the modification of N‐heterocyclic scaffolds of appealing ligands and pharmaceuticals.