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Updated: Jun 17, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Amine Transaminase-Catalyzed Enantioselective Synthesis of Cyclohexylidene-Based Axially Chiral Amines
Haiyan Xu1,2,3, Lin Yang3,4, Li Zhang1,2
1School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, P. R. China.
Abstract:
We report an unprecedented amine transaminase-catalyzed asymmetric transamination of 4-alkylidene cyclohexanones, affording various axially chiral alkylidene cyclohexane amines in high conversions (up to 99%) and excellent stereoselectivities (mostly between 96% and 99% ee). The synthetic prospect was underscored further by efficient preparative-scale synthesis (67-83% isolated yields) and downstream product derivatization. Molecular dynamics simulations and related mutational studies were conducted to gain insights into effective catalysis, including the rationale for the superb observed enantioselectivity.
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