Synthesis of Heterocycle‐fused Pyridine N‐Oxides from Oximes and Diazo Compounds via RhIII‐Catalyzed CH Activation and Annulation

A RhIII‐catalyzed tandem CH activation and CN bond formation reaction between oximes and diazo compounds for the synthesis of heterocycle‐fused pyridine N‐oxides has been developed. The reaction exhibits good functional group tolerance and regioselectivity. After simple transformation, the 1‐substituted, 1,3‐disubstituted, 1,4‐disubstituted and 1,3,4‐trisubstituted heterocycle‐fused pyridines were all obtained in high efficiency. Moreover, this strategy has also been expanded to the synthesis of a key intermediate for the construction of one potential anti‐HIV agent. magnified image