Nitrilase mutant and application thereof in preparation of anti-epileptic drug intermediate

A technology of nitrilase and mutants, applied in the directions of immobilization on or in inorganic carriers, hydrolase, immobilization on/in organic carriers, etc., can solve the problems of poor thermal stability and low catalytic activity of catalyst enzymes
CN111172140AActive Publication Date: 2020-05-19ZHEJIANG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2020-05-19

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Abstract

The invention discloses a nitrilase mutant and an application thereof in preparation of an anti-epileptic drug intermediate. The mutant is obtained by mutating one or more of 151th amino acid, 223th amino acid and 250th amino acid of an amino acid sequence shown in SEQ ID No.2. The thermal stability of the nitrilase mutant AcN-T151V / C223A / C250G is improved by 1.73 times, 1M 1-cyanocyclohexyl acetonitrile is hydrolyzed by use of recombinant escherichia coli containing the nitrilase mutant at the temperature of 35 DEG C to generate 1-cyanocyclohexylacetic acid, and the yield of a final product reaches 95%. When 1.2 M 1-cyanocyclohexyl acetonitrile is hydrolyzed at the temperature of 35 DEG C, the final yield reaches 97%. Gabapentin is synthesized by use of the nitrilase mutant, and the yieldof the final product reaches 80%.
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Description

[0001] (1) Technical field

[0002] The invention relates to a mutant derived from nitrilase of Acidovorax facilis CCTCC NO:M 209044 and its application in the synthesis of 1-cyanocyclohexylacetic acid, an intermediate of antiepileptic drugs.

[0003] (2) Background technology

[0004] Gabapentin is a new type of antiepileptic drug first developed by Warner-Lambert Company of the United States. Compared with similar drugs currently on the market, it has the advantages of fast oral absorption, less toxic and side effects, obvious therapeutic effect and strong tolerance. The blood-brain barrier of the human brain is less likely to interact with other antiepileptic drugs, and its effect as a superimposed drug for intractable epilepsy is particularly prominent.

[0005] 1-cyanocyclohexylacetic acid is a key intermediate in the synthesis of antiepileptic drug gabapentin, and it has broad application prospects in the market. At present, the industrial synthesis of gabapentin and th...

Claims

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