Diversity‐Oriented Synthesis of Functionalized Imidazopyridine Analogues with Anti‐Cancer Activity through a Transition‐Metal Free, One‐pot Cascade Reaction

Abstract A transition‐metal free, high yielding and efficient three‐component reaction was designed and incorporated into two sequential oxidation and cyclization reaction cascades in one‐pot with the assistance of microwave irradiation. A chemical collection of functionalized 3‐substituted imidazopyridines was prepared by means of the mild reaction and simple operational procedure. The reaction has a broad tolerance for a variety of substituted carbonyl aldehydes, anilines and 2‐phenyl‐imidazo[1,2‐ a ]pyridines. Screening in several cancer cell lines was conducted. Compound 9 i exhibited good potency against HeLa cell lines and this work validated the feasibility of the methodology for generating bioactive compounds. magnified image