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Enantioselective synthesis of 3-arylindole atropisomers via organocatalytic indolization of iminoquinones

Yuwei Liu, Ye‐Hui Chen, Jun Kee Cheng, Shao‐Hua Xiang, Bin Tan

2023Chemical Synthesis29 citationsDOIOpen Access PDF

Abstract

The direct enantioselective construction of axially chiral 3-arylindole frameworks via nucleophilic addition of 2-substituted indoles to iminoquinones has been achieved with high efficiencies under mild chiral phosphoric acid (CPA) catalytic conditions. The utility of this method was demonstrated in successful scale-up syntheses without compromising the product yields and enantioselectivities. The oxidation of products yields axially chiral heteroaryl-p-quinone monoimine, which could be subjected to structural diversification via addition of nucleophiles.

Topics & Concepts

Enantioselective synthesisAtropisomerNucleophilePhosphoric acidChemistryCatalysisCombinatorial chemistryOrganic chemistryAxial and Atropisomeric Chirality SynthesisNonlinear Waves and SolitonsAlgebraic structures and combinatorial models
Enantioselective synthesis of 3-arylindole atropisomers via organocatalytic indolization of iminoquinones | Litcius