Rhizopus microsporus root-shaped variant ZJPH1308 and application thereof in preparation of sitagliptin intermediate

A kind of technology of Rhizopus microspora and varieties, applied in the field of application of Rhizopus microspora whisker variety ZJPH1308 and in the preparation of sitagliptin intermediates
CN104893989AActive Publication Date: 2015-09-09JIANGSU TIANHE PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANGSU TIANHE PHARMA CO LTD
Publication Date
2015-09-09

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Abstract

The invention discloses a rhizopus microsporus root-shaped variant ZJPH1308 and application thereof in preparation of a sitagliptin intermediate. A strain of the rhizopus microsporus root-shaped variant ZJPH1308 can be used for biologically and asymmetrically reducing 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazol[4,3-a]pyrazine-7-(8H)-yl]-1-(2,4,5-trifluorophenyl)butanone so as to obtain (S)-3-hydroxyl-1-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazol[4,3-a]pyrazine-7-(8H)-yl]-4-(2,4,5-trifluorophenyl)butanone. The strain has the advantages of good three-dimensional selectivity, high product optical purity and the like. The rhizopus microsporus root-shaped variant ZJPH1308 is fermented and cultured to obtain a wet thallus which serves as chiral biological catalyst; when the substrate concentration is 10mmol / L, the reduction product yield is as high as 95%, and the e.e. value of the product is greater than 99.9%.
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Description

(1) Technical field

[0001] The present invention relates to the preparation of a sitagliptin intermediate, in particular to a new strain--Rhizopus microsporus var.rhizopodiformis ZJPH1308, and its asymmetric synthesis of sitagliptin by microorganism catalysis Chiral Intermediate (S)-3-Hydroxy-1-[3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine -7-(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one. (2) Background technology

[0002] Sitagliptin (Sitagliptin, trade name ), the chemical name is (3R)-3-amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3- a] pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one, the first dipeptidyl peptidase-4 (DPP- 4) Inhibitors for the treatment of type II diabetes. The drug has the functions of protecting pancreatic beta cells, slowing down the activity inhibition of hypoglycemic hormones, and regulating blood sugar in patients with type II diabetes. It was approved for marketing by the US Food and Drug Administratio...

Claims

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