Engineering a Carbonyl Reductase for Scalable Preparation of (S)-3-Cyclopentyl-3-hydroxypropanenitrile, the Key Building Block of Ruxolitinib,ChemBioChem

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Engineering a Carbonyl Reductase for Scalable Preparation of (S)-3-Cyclopentyl-3-hydroxypropanenitrile, the Key Building Block of Ruxolitinib
ChemBioChem ( IF 2.6 ) Pub Date : 2021-12-23 , DOI: 10.1002/cbic.202100589
Yunfeng Cui ₁ , Liangyan Zhu _{1,

2} , Xi Chen _{1,

2} , Jinhui Feng ₁ , Qiaqing Wu _{1,

2} , Dunming Zhu ₁

Affiliation

Rational engineering of the carbonyl reductase PhADH resulted in a double mutant H93C/A139L, which enhanced the enantioselectivity toward the reduction of 3-cyclopentyl-3-ketopropanenitrile 1 a from 85 % to 99 %, as well as a 6-fold improvement in the specific activity. (S)-3-Cyclopentyl-3-hydroxypropanenitrile ((S)-1 b) was prepared at 200 g/L (1.5 M) substrate concentration.

中文翻译：

设计用于可扩展地制备 (S)-3-Cyclopentyl-3-羟基丙腈（鲁索替尼的关键构件）的羰基还原酶

羰基还原酶 PhADH 的合理工程产生了双突变体 H93C/A139L，这增强了对映选择性将 3-环戊基-3-酮丙腈1a从 85 % 还原到 99 %，并提高了 6 倍具体活动。( S )-3-环戊基-3-羟基丙腈 (( S ) -1b ) 以 200 g/L (1.5 M) 底物浓度制备。

更新日期：2021-12-23

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