Cycloaddition Reaction of N-Homoallylacetohydrazides with O-Benzoylhydroxylamines under Copper Catalysis: Access to Tetrahydropyridazine Skeletons

Org Lett. 2025 Jul 3. doi: 10.1021/acs.orglett.5c02156. Online ahead of print.

Abstract

We present a practical copper-catalyzed strategy for the amination and cyclization of unactivated alkenes. The transformation employs O-benzoylhydroxylamines as alkylamine precursors to initiate a radical cascade process. This protocol enables the construction of a diverse array of tetrahydropyridazine scaffolds by reacting N-homoallylacetohydrazides with O-benzoylhydroxylamines, ultimately affording a total of 25 structurally varied derivatives.