Regio‐Selective C−H Halogenation of 8‐Amido‐Quinolines under Transition Metal Free Conditions

Abstract

Abstract A transition metal free highly regioselective remote C−H 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 N‐halosuccinimide (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.