Rhodium-Catalyzed C-H Activation/Annulation Cascade of Aryl Oximes and Propargyl Alcohols to Isoquinoline N-Oxides

A beta-hydroxy elimination instead of common oxidization to carbonyl group in secondary propargyl alcohols was successfully developed to form 2-benzyl substituted isoquinoline N-oxides by a Rhodium-catalyzed C-H activation and annulation cascade, in which moderate to excellent yields (up to 92%) could be obtained under mild reaction conditions, along with good regioselectivity, broad generality and applicability.

Automated summary

The study developed a beta-hydroxy elimination approach for the synthesis of 2-benzyl substituted isoquinoline N-oxides from secondary propargyl alcohols, achieving moderate to excellent yields (up to 92%) under mild reaction conditions, with good regioselectivity, broad generality, and applicability.