Metal-free C5-selective halogenation of quinolines under aqueous conditions

摘要

An efficient and convenient method of C5-selective halogenation of quinoline derivatives was developed. The reaction proceeds smoothly in water with readily available N-halosuccinimides (NCS, NBS and NIS) as the halogenation reagents. This method features metal-free catalysis, no additional oxidants and additives, broad substrate scope and short reaction time.