Aug 2026· ChemCatChem· Vol 18· 0 citations· 42 references
Abstract
Enantioselective transamination of prochiral ketones is an indispensable transformation in the pharmaceutical and fine chemical industries. Transaminases have emerged as valuable biocatalysts for the preparation of a wide range of chiral amines through either kinetic resolution or asymmetric synthesis. Here, we explored the synthetic potential of the engineered amine transaminase 3FCR‐4M through systematic evaluation of combinatorial variants in both kinetic resolution and asymmetric synthesis mode. This dual assessment not only revealed synergistic effects between individually beneficial mutations, but also offered insight into the limited predictive value of kinetic resolution activity for asymmetric synthesis efficiency. Notably, we report for the first time the transaminase‐catalyzed direct amination of a terminal alkyne‐bearing substrate. The transamination of 1‐(4‐ethynylphenyl)ethanone proceeded with >99% conversion and excellent enantioselectivity (>99%ee), opening a new perspective for the integration of transaminase catalysis into click chemistry‐based synthetic workflows.
Nowadays, there is a growing need for streamlined and sustainable strategies to access chiral nitrogen heterocycles, whose stereodefined frameworks underpin their broad functional and pharmaceutical relevance. Herein, we report a robust continuous flow enzymatic protocol for the stereoselective synthesis of the natur...
Sara Vicinanza, Ilaria Magrini Alunno, Stefania Patti et al.· Advanced Synthesis & Cat...· 0 citations
Chiral arylvinyl-substituted 3-hydroxy-5-oxo esters are valuable motifs in pharmaceuticals, yet their enantiocontrolled synthesis remains challenging. Herein, we report a biocatalytic system using ketoreductases (KREDs) for the highly C3-selective reduction of arylvinyl-substituted 3,5-dicarbonyl esters. Through semira...
Xiao-Qiu Wu, Ming-Yu Zhang, Ming-Yang Yao et al.· Organic Letters· 0 citations
Atropisomeric compounds are widely distributed in natural products and pharmaceuticals and serve as key scaffolds in asymmetric catalysis. Despite their remarkable structural diversity, current synthetic efforts have primarily focused on C–C biaryl atropisomers, while the synthesis of other classes of atropisomeric com...
Axially chiral biaryl dimethanols are ubiquitous and multifunctional intermediates for the synthesis of valuable atropisomeric molecules in advanced materials, drugs, natural products, and organocatalysts. Despite their broad synthetic utility, direct enantiodivergent catalytic access to this specific class of compou...
Jie Chen, Zhuoting Peng, Xiaolong Gao et al.· ACS Catalysis· 0 citations
Axially chiral amines embedded in rigid spirocyclic frameworks are valuable motifs in medicinal chemistry, yet their synthesis by direct asymmetric amination of sterically congested ketones remains highly challenging. Here, we report an engineered ω-transaminase variant for the direct asymmetric amination of 2,6-disu...
Zi-Yi Lin, Meijiao Gao, Qikai Sun et al.· ACS Catalysis· 0 citations
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