Regioselective C3–H Alkylation of Imidazopyridines with Donor–Acceptor Cyclopropanes

Alkylated imidazopyridines are crucial structures for medicinal chemistry. Here, an efficient method for the C3–H alkylation of imidazopyridines was devised. Under Lewis acid-catalyzed conditions, reactions of imidazopyridines with different donor–acceptor cyclopropanes were carried out. Finally, 1,3-bisfunctionalizaton of donor–acceptor cyclopropanes was performed. In addition, synthesized C3-alkylated imidazopyridines are amenable for diverse synthetic applications.