Recent Advances in Organocatalytic Kinetic Resolution for the Synthesis of Axially Chiral Compounds
Liying Cui, Yin Zheng
TL;DR
This review highlights recent progress in using organocatalytic methods to efficiently synthesize axially chiral compounds, which are important in chemistry and drug development.
Contribution
The paper provides a comprehensive overview of advances in organocatalytic kinetic resolution for axially chiral compound synthesis from 2010 to 2025.
Findings
Organocatalytic kinetic resolution (OKR) has improved the synthesis of axially chiral compounds through better catalyst design and stereocontrol.
Non-covalent interactions in OKR enable sustainable and enantioselective synthesis of C–C biaryl, C–N heterobiaryl, and olefinic frameworks.
The review identifies current challenges and future directions in the development of OKR methods.
Abstract
Axially chiral compounds, indispensable in asymmetric catalysis, drug discovery, and materials science, have witnessed transformative advancements in synthesis through organocatalytic kinetic resolution (OKR) over the past decade. This review systematically dissects the latest achievements (2010–2025) in OKR, focusing on catalyst design, mechanistic insights, substrate diversification, and synthetic applications across C–C biaryl, C–N heterobiaryl, and olefinic axially chiral frameworks. By harnessing non-covalent interactions, OKR has emerged as a powerful strategy to overcome the challenges of low rotational barriers and limited stereocontrol, offering sustainable and enantioselective access to privileged chiral scaffolds. Furthermore, the current challenges and future prospects in this rapidly evolving field are assessed.
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Taxonomy
TopicsAxial and Atropisomeric Chirality Synthesis · Asymmetric Synthesis and Catalysis · Synthesis and Properties of Aromatic Compounds