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Organocatalytic Atroposelective Construction of Axially Chiral <i>N</i>-Aryl Benzimidazoles Involving Carbon–Carbon Bond Cleavage

Ningning Man, Zhenbang Lou, Yuming Li, Haijun Yang, Yufen Zhao, Hua Fu

2020Organic Letters54 citationsDOI

Abstract

Axially chiral compounds widely occur in natural products, biologically active molecules, ligands, and catalysts, and their efficient and enantioselective synthesis is highly desirable. Herein, we report a novel method for the atroposelective construction of axially chiral N-aryl benzimidazoles with chiral phosphoric acid as the organocatalyst via reaction of N1-(aryl)benzene-1,2-diamines with multicarbonyl compounds. The present method provided the target products in high yields (up to 89%) with excellent enantioselectivity (up to 98% ee).

Topics & Concepts

ChemistryArylEnantioselective synthesisPhosphoric acidAxial symmetryCatalysisCombinatorial chemistryAxial chiralityMoleculeBenzeneOrganic chemistryStructural engineeringAlkylEngineeringAxial and Atropisomeric Chirality SynthesisMolecular spectroscopy and chiralitySphingolipid Metabolism and Signaling
Organocatalytic Atroposelective Construction of Axially Chiral <i>N</i>-Aryl Benzimidazoles Involving Carbon–Carbon Bond Cleavage | Litcius