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Intermolecular Vicinal Diaminative Assembly of Tetrahydroquinoxalines via Metal-free Oxidative [4 + 2] Cycloaddition Strategy

Dangui Wang, Huaibin Yu, Shao-Han Sun, Fangrui Zhong

2020Organic Letters42 citationsDOI

Abstract

-phenylenediamines with various alkenes. Differing from the known strategy that hinged on reactive π-allyl Pd intermediates from restrained allylic alcohol/acetate and diene substrates, this metal-free method features easy accessibility of starting materials, step economy, benign reaction conditions, and more importantly broad C-C double bonds (styrenes, vinyl (thio)ethers, benzofurans, indoles) with diastereospecificities. Mechanistic studies suggest the intermediacy of the benzoquinone diimides, a class of useful but yet underexploited synthons. Of note, they efficiently furnished functionalized tetrahydroquinoxalines and complement the well-studied alkene vicinal diamination typically toward acyclic diamine derivatives.

Topics & Concepts

VicinalChemistryIntermolecular forceCycloadditionOxidative phosphorylationMetalCombinatorial chemistryComputational chemistryMoleculeOrganic chemistryCatalysisBiochemistryOxidative Organic Chemistry ReactionsSynthesis and Catalytic ReactionsCatalytic C–H Functionalization Methods
Intermolecular Vicinal Diaminative Assembly of Tetrahydroquinoxalines via Metal-free Oxidative [4 + 2] Cycloaddition Strategy | Litcius