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Rhodium(III)-Catalyzed Atroposelective Synthesis of C–N Axially Chiral Naphthylamines and Variants via C–H Activation

Peiyuan Wang, Yaling Huang, Jierui Jing, Fen Wang, Xingwei Li

2022Organic Letters53 citationsDOI

Abstract

Reported herein is the efficient and atroposelective construction of two categories of C-N atropisomers via rhodium(III)-catalyzed C-H activation of sulfoxonium ylides en route to [4+2] annulation with sterically hindered, electron-rich alkynes. This reaction proceeds with high regio- and enantioselectivity under redox-neutral conditions via a double-substrate activation strategy, providing a novel entry to C-N axially chiral 4-functionalized 1-naphthols.

Topics & Concepts

AtropisomerChemistryAnnulationRhodiumCatalysisSteric effectsSubstrate (aquarium)StereochemistryCombinatorial chemistryYield (engineering)Medicinal chemistryOrganic chemistryMaterials scienceGeologyMetallurgyOceanographyAxial and Atropisomeric Chirality SynthesisCatalytic C–H Functionalization MethodsAlkaloids: synthesis and pharmacology
Rhodium(III)-Catalyzed Atroposelective Synthesis of C–N Axially Chiral Naphthylamines and Variants via C–H Activation | Litcius