Recent advances in the construction of C-N axial chirality via asymmetric C-H activation

Junlian Ji

Jun Wang

*Correspondence to: Jun Wang, Key Laboratory of Bioinorganic and Synthetic Chemistry of Ministry of Education, School of Chemistry, and Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, Sun Yat-sen University, Guangzhou 510006, Guangdong, China. E-mail: wangjun23@mail.sysu.edu.cn

Chiral Chem. 2027;3:202635. 10.70401/cc.2026.0046

Received: July 27, 2026Accepted: October 28, 2026Published: October 28, 2026

This manuscript is made available in its unedited form to allow early access to the reported findings. Further editing will be completed before final publication. As such, the content may include errors, and standard legal disclaimers are applicable.

Abstract

C-N chiral axes are prevalent in natural products, bioactive molecules, and chiral ligands. The development of synthetic methodologies for constructing C-N chiral axes has attracted considerable interest among chemists. Herein, we review advances in the construction of C-N axial chirality via asymmetric C-H activation, a strategy with high atom- and step-economy. This review covers the literatures from 2019 to 2026, categorizing the transformations into annulation, alkynylation, alkenylation, alkylation, arylation, borylation and imidoylation. The representative products, reaction mechanisms, and the application of products are demonstrated. We hope this review will serve as a useful guide for chemists interested in this field and stimulate further progress in this area.

Keywords

C-N Axial chirality, C-H activation, asymmetric catalysis

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Ji J, Wang J. Recent advances in the construction of C-N axial chirality via asymmetric C-H activation. Chiral Chem. 2027;3:202635. https://doi.org/10.70401/cc.2026.0046