Synthesis of Substituted Pyrido[1,2‐a]benzimidazoles by Ruthenium‐Catalyzed C−H Bond Activation and Tandem Cyclization of 2‐Arylimidazo[1,2‐a]pyridines with Iodonium Ylides

Abstract Ruthenium‐catalyzed C−H bond activation and tandem cyclization of 2‐arylimidazo[1,2‐ a ]pyridines with iodonium ylides proceed efficiently. For the first time, the easily available iodonium ylides and inexpensive ruthenium complex were employed to synthesize pyrido[1,2‐ a ]benzimidazole derivatives in good yields under simple and easy‐to‐operate conditions. Several primary mechanism investigations and synthetic applications involving gram‐scale preparation, derivatization reactions and the transformation of iodonium ylide generated in situ have also been conducted.