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An efficient protocol to synthesize substituted benzo[4,5]imidazo[1,2- c]quinazolines starting from N-LG-2-phenylbenzoimidazole and dioxazolones catalyzed by Rh(III) or Ir(III) has been developed. Various substituted benzo[4,5]imidazo[1,2- c]quinazolines could be easily provided in up to 99% yield. A large range of substrates and functional groups are compatible for this transformation. This method features low catalyst loading, acid-free conditions, and low solvent consumption.

An efficient tandem reaction of imidamides and N-hydroxycarbamates has been developed. Valuable 2-alkylbenzimidazoles could be easily obtained in up to 97% yield for more than 20 examples. The products would further streamline the synthesis of molecules, which are essential building blocks in organic synthesis and drug discovery. This protocol features high regioselectivity, efficiency, good tolerance of functional groups, and mild reaction conditions.

A novel Ir-catalyzed annulation of imidamides with sulfonyl azides has been developed. 1,2-Disubstituted benzimidazoles could be easily obtained in up to 99% yield for more than 40 examples. The products further streamline the synthesis of molecules that are important building blocks for organic synthesis and drug discovery. This strategy features high regioselectivity, efficiency, good tolerance of functional groups, and mild reaction conditions.

Ir-catalyzed direct C-H sulfamidation of benzaldehydes has been achieved. A series of ortho-amided benzaldehydes were obtained in up to 95% yields for 21 examples with excellent regioselectivity and broad functional group tolerance. This transformation could proceed smoothly with low catalyst loading under external-oxidant-, acid-, or base-free conditions. Molecular nitrogen was released as the sole byproduct, providing an environmentally benign sulfamidation process.