Metal‐Free, H2O2‐Mediated, Regioselective Direct C‐3 Hydroxylation of Imidazo[1,2‐a]pyridines via C(sp2)‐H Bond Functionalization

Abstract For the first time, a new, cost‐effective, metal‐free, H 2 O 2 (50 % in water)‐mediated regioselective direct C‐3 hydroxylation of imidazo[1,2‐ a ]pyridines via C‐H bond functionalization is reported. This metal‐free C (sp 2 ) ‐O bond formation protocol is operationally simple and showed broad range of functional group tolerance and substrate affinity. To the best of our knowledge, this is the first report of imidazo[1,2‐ a ]pyridine‐3‐ols showing promising in vitro antioxidant activity.