Synthesis of Heterocycle-fused Pyridine N-Oxides from Oximes and Diazo Compounds via Rh-III-Catalyzed CH Activation and Annulation

摘要

A Rh-III-catalyzed tandem CH activation and CN 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.