We report here a generic, green synthesis of 17 valuable syn-aryl-(2S,3R)-2‑chloro-3‑hydroxy esters (syn-(2S,3R)-1) in 73%-99% isolated yields along with 6.1:1–83:1 dr and 31%∼>99% ee, through dynamic reductive kinetic resolution of racemic aryl α‑chloro β-keto esters (2) catalyzed by an engineered ketoreductase which was obtained via epPCR-based directed evolution. The hectogram scale synthesis of syn-(2S,3R)-1b at a substrate concentration of 120 g/L showcased the application potential of the biocatalytic method developed presently.

中文翻译：

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通过工程酮还原酶催化的动态还原动力学拆分不对称合成顺芳基-(2S,3R)-2-氯-3-羟基酯

我们在此报道了 17 种有价值的顺式芳基-(2S , 3R ) -2-氯-3-羟基酯 ( syn- (2S , 3R ) -1 )的通用绿色合成方法，合成率为 73%-99%通过由epPCR获得的工程酮还原酶催化的外消旋芳基α -氯β -酮酯 ( 2 )的动态还原动力学拆分，分离出的产量为 6.1:1–83:1 dr和 31%∼>99% ee 。基于定向进化。syn -(2 S ,3 R )- 1b的百克级合成底物浓度为120 g/L时显示了目前开发的生物催化方法的应用潜力。