Ketoreductase RasADH-E189D and application thereof

By using ketone reductase to catalyze the asymmetric reduction reaction of aryl-substituted alkenyl 3,5-dicarbonyl esters, the problem of the difficulty in efficiently preparing chiral β-hydroxy esters in the existing technology has been solved, achieving a biocatalytic effect with high selectivity and high conversion rate, and successfully synthesizing pitavastatin intermediates.

CN122128264AActive Publication Date: 2026-06-02SHANGHAI OCEAN UNIV
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Patent Information

Application Number
CN202610620943.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-05-08
Publication Date
2026-06-02
Estimated Expiration
2046-05-08

AI Technical Summary

Technical Problem

Existing methods are insufficient to efficiently achieve highly selective asymmetric reduction of aryl-substituted alkenyl 3,5-dicarbonyl esters to prepare chiral β-hydroxy esters without pre-reduction, protection, or pre-functionalization of the substrate.

Method used

A biocatalytic platform was constructed to prepare high-purity chiral aryl-substituted alkenyl β-hydroxy esters by using ketone reductases RasADH, RasADH-E189D, KmCR2, SSCR-QA, or SSCR-QA to catalyze the asymmetric reduction reaction of aryl-substituted alkenyl 3,5-dicarbonyl esters.

Benefits of technology

Highly selective asymmetric reduction of aryl-substituted alkenyl 3,5-dicarbonyl esters was achieved with a conversion rate of 89%-99% and an enantioselectivity of 93%-99%. Key intermediates of pitavastatin were also successfully prepared, exhibiting good diastereoselectivity.

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Abstract

The invention provides ketoreductase RasADH-E189D and application of the ketoreductase RasADH-E189D The RasADH-E189D enzyme is obtained through a site-specific mutagenesis technology, and the amino acid sequence of the RasADH-E189D enzyme is shown as SEQ ID NO. 4. The RasADH-E189D can efficiently catalyze an asymmetric reduction reaction of aryl substituted alkenyl 3, 5-dicarbonyl ester with high stereoselectivity, so that high-purity chiral aryl substituted alkenyl beta-hydroxy ester is prepared, and the RasADH-E189D has important application value in the field of chiral drug synthesis.
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