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Construction of Axially Chiral Styrenes Linking an Indole Moiety by Chiral Phosphoric Acid

Wenxuan Zhang, Ran Song, Daoshan Yang, Jian Lv

2022The Journal of Organic Chemistry35 citationsDOI

Abstract

Herein we report a chiral phosphoric acid-catalyzed intermolecular C2 Friedel–Crafts alkylation reaction between ortho-alkynylnaphthols and various 3-substituted indoles, affording axially chiral alkenes with up to 93% yields (E/Z > 20:1) and up to 98% ee under mild reaction condition. Other substituted indole derivatives could be also tolerated in this system, giving the corresponding axially chiral alkenes with high yields and in excellent enantioselectivity.

Topics & Concepts

Phosphoric acidMoietyIndole testAxial symmetryChemistryFriedel–Crafts reactionAlkylationOrganic chemistryCatalysisIntermolecular forceMoleculePhysicsQuantum mechanicsAxial and Atropisomeric Chirality SynthesisMolecular spectroscopy and chiralityAlgebraic structures and combinatorial models
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