The asymmetric synthesis of atropisomers has garnered extensive attention in recent years. Atropisomers constitute a key structural motif in natural products, chiral ligands, organocatalysts, and functional materials. Despite progress driven by transition‐metal and organocatalysis, inherent limitations in enantioselectivity and sustainability have hampered further development in this field. Alternatively, biocatalysis offers a promising solution employing strategies including (dynamic) kinetic resolution, desymmetrization, and other strategies. These biocatalytic processes operate under mild, environmentally friendly conditions, achieving high stereoselectivity that is often difficult to attain with traditional methods. This review highlights recent advances in the biocatalytic synthesis of atropisomers and offer insights in the development of the relevant field.
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Zhoutong Sun (2025) studied this question.
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