Transaminase mutant and applications of transaminase mutant in Sitagliptin synthesis

A mutant and transaminase technology, applied in the fields of genetic engineering and enzyme catalysis, can solve the problems of expensive reagents, chiral catalysts and chiral auxiliary agents, etc., and achieve the effect of improving enzyme activity
CN112094856AActive Publication Date: 2020-12-18SHANXI WEIQIDA PHARMA IND
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
SHANXI WEIQIDA PHARMA IND
Publication Date
2020-12-18

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Abstract

The invention discloses a mutant of transaminase SEQ ID NO: 1. The mutant has significantly enhanced enzyme activity and high stereoselectivity; the mutant can efficiently catalyze (2Z)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine-7-(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-one to synthesize the Sitagliptin, and the e.e. value of products is greater than 99.95%, so thatthe mutant has industrial application prospects.
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Description

technical field

[0001] The invention belongs to the technical field of genetic engineering and enzyme catalysis, and in particular relates to a transaminase mutant and its application in the synthesis of sitagliptin. Background technique

[0002] Sitagliptin, also known as sitagliptin, its full name is 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5 ,6,7,8-tetrahydro-3-trifluoromethyl-1,2,4-triazolo[4,3-a]pyrazine is the first dipeptide developed by Merck DPP-4 inhibitors, and their phosphorylated hydrates are currently type II diabetes drugs that occupy a huge market share.

[0003] In the synthetic route of sitagliptin, the introduction of chiral (R)-amino group is one of the key steps. At present, methods including chiral source introduction, selective reduction, chiral induction and kinetic resolution have been developed. Among them, (2Z)-4-oxo-4-[3-(trifluoromethyl)-5,6- Dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7-(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2- Keton...

Claims

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