Synthesis of Dihydropyrazoles via Palladium‐Catalyzed Cascade Heterocyclization/Carbonylation/Arylation of β,γ‐Unsaturated N‐Tosyl Hydrazones

Abstract

AbstractA Pd‐catalyzed heterocyclization/carbonylation/arylation cascade reaction between β,γ‐unsaturated N−Ts hydrazones and commercially available arylboronic acids as coupling partners is described, producing 2‐pyrazoline‐ketone derivatives in 11–78% yield. A detailed statistical analysis of reactivity patterns of boronic acids provided key information about the limitations of the method, highlighting the challenges of degradation pathways. Our methodology offers a tool for synthesizing diverse 2‐pyrazoline‐ketone derivatives, expanding the toolbox of accessible N−N‐heterocycles.