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Synthesis of Dihydropyrazoles via Ligand-Free Pd-Catalyzed Alkene Aminoarylation of Unsaturated Hydrazones with Diaryliodonium Salts

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posted on 2017-09-12, 19:07 authored by Meng-Nan Yang, Dong-Mei Yan, Quan-Qing Zhao, Jia-Rong Chen, Wen-Jing Xiao
A ligand-free, palladium-catalyzed aminoarylation reaction of the unactivated alkenes in β,γ-unsaturated hydrazones is described. This protocol enables efficient and simultaneous formation of C­(sp3)–N and C­(sp3)–C­(sp2) bonds under mild conditions, providing a practical and general approach to various diversely substituted dihydropyrazoles in generally good yields, without the use of any stoichiometric external oxidant.

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