An improved cyanoreductase and its application in the synthesis of 3-chloropyrazine-2 methylamine

A technology of cyanopyrazine and reductase, which is applied in the direction of enzymes, biochemical equipment and methods, fermentation, etc., can solve the problems of large amount of organic solvent usage, heavy metal pollution, high production cost, etc. The effect of system green environmental protection and performance improvement
CN109182286BActive Publication Date: 2021-07-30泰州学院
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
泰州学院
Publication Date
2021-07-30

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Abstract

The invention discloses an improved cyano reductase and its application in the synthesis of 3-chloropyrazine-2 methylamine, characterized in that: the improved cyano reductase is represented by SEQ ID No.2 The amino acid sequence is the starting sequence, the mutant obtained by mutating the 120th alanine to leucine, and mutating the 155th glutamic acid to lysine; Add glucose, coenzyme NADP, 2-chloro-3-cyanopyrazine, glucose dehydrogenase and improved cyanoreductase to form a reaction mixture, and carry out the reduction reaction at 30-40°C for 24 hours to generate 3-chloropyrazine -2 methylamine, the present invention has mild reaction conditions, less organic solvent consumption, more green reaction system, high conversion rate, greatly improves the preparation efficiency of 3-chloropyrazine-2 methylamine, and has good industrial application prospect.
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Description

technical field

[0001] The invention belongs to the field of biocatalysis, and in particular relates to an improved cyanoreductase and its application in synthesizing 3-chloropyrazine-2 methylamine. Background technique

[0002] 3-Chloropyrazine-2-methylamine is the key intermediate of Acalabrutinib, a second-generation Bruton's tyrosine kinase (BTK) inhibitor developed by Acerta , can promote durable high response rates in patients with chronic lymphocytic leukemia (CLL). In 2017, the drug was approved by the FDA for the indication of mantle cell lymphoma.

[0003] At present, there are many reports on the synthesis of 3-chloropyrazine-2 methylamine by chemical methods, mainly using 2-chloro-3-cyanopyrazine as raw material, and 3-chloropyrazine-2 methylamine is obtained through reduction. This type of method uses a large amount of organic solvents, many operating links, a long preparation period, low yield, heavy metal pollution, and high production costs. Compared with ...

Claims

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