Research Progress on Organocatalytic Asymmetric Synthesis of Atropisomeric Aldehydes

The burgeoning field of asymmetric catalysis has significantly advanced the construction of axially chiral compounds, recognized for their distinct three‐dimensional structures that are relevant in drug discovery, catalyst design and material science. Particularly, the atropisomeric aldehydes, characterized by a chiral axis and the presence of an aldehyde functionality, are of increasing value and interest in chemistry‐related domains, such as serving as privileged chiral catalysts for activation of amines. In recent years, elegant environmentally‐friendly metal‐free catalytic asymmetric methodologies based on de novo formation of (hetero)aromatic rings, dynamic kinetic resolution and desymmetrization have been established to build this fascinating class of atropisomers. In this review, we would like to highlight recent research progress on enantioselective synthesis of atropisomeric aldehydes by means of organocatalysis and biocatalysis, including their scopes, limitations, mechanisms, synthetic applications and provide some insights into future development. 1. Introduction 2. Ring Formation 3. Dynamic Kinetic Resolution 4. Desymmetrization 5. Conclusions and Outlook 6. References