Regio-Selective CH Halogenation of 8-Amido-Quinolines under Transition Metal Free Conditions

摘要

A transition metal free highly regioselective remote CH halogenation has been developed. Oxidative halogenation (Cl, Br, I) of C5-H of 8-amido quinolone with inexpensive potassium persulfate as an oxidant and cheap halogenating agents like Nhalosuccinimide (NXS) or tetrabutylammonium halides (TBAX) were employed. Two reaction conditions were developed and in both routes have advantages such as C5-selectivity, high to excellent yields (up to 98%) and broad substrate scope. The reaction also carried out in water, open to air condition.