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

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. (Figure presented.).