一种羰基还原酶突变体及其在合成(R)-3-氯苯丙醇中的应用
By modifying the carbonyl reductase LkSDR and optimizing the catalytic reaction system, the problems of insufficient catalytic activity and stereoselectivity of (R)-3-chlorophenylpropanol in the existing technology were solved, realizing a highly efficient, green and environmentally friendly bio-enzymatic synthesis, with significantly improved product optical purity and yield.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Filing Date
- 2026-06-18
- Publication Date
- 2026-07-17
AI Technical Summary
Existing chemical methods for synthesizing the dapoxetine intermediate (R)-3-chlorophenylpropanol suffer from low catalytic activity and insufficient stereoselectivity, resulting in low yields and difficulty in achieving the required optical purity for pharmaceutical applications. Bioenzymatic methods require high-cost chiral catalysts and are prone to dechlorination reactions in aqueous systems.
By molecularly modifying the carbonyl reductase LkSDR, a carbonyl reductase mutant with high activity and high stereoselectivity was obtained. Combined with glucose dehydrogenase and an optimized catalytic reaction system, (R)-3-chlorophenylpropanol was efficiently synthesized in the aqueous phase using the inexpensive coenzyme NAD+.
High yield and high optical purity of (R)-3-chlorophenylpropanol were achieved, with an eep value of 99%, few byproducts, and the process was green, environmentally friendly, and economically feasible, avoiding the use of high-concentration co-solvents.
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Figure CN122405575A_ABST