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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N1-02
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filingDate 2022-02-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7aaeb21aba353408472d818a39199369
publicationDate 2022-05-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-114507699-A
titleOfInvention A kind of low-cost preparation method of sitagliptin phosphate
abstract The invention relates to a low-cost preparation method of sitagliptin phosphate, belonging to the field of medicine and chemical industry. The content includes providing a strain, screening of carbonyl reductase-producing strains, reduction of substrates, immobilization of cells by embedding method, preparation of sitagliptin, and preparation of sitagliptin phosphate. The carbonyl reductase of the present invention catalyzes the reduction of 4-oxy-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 (I), followed by cell immobilization to achieve (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‑ketone (II) is efficiently and selectively prepared, so that the yield and ee value of sitagliptin phosphate are both greater than 99%, and the method has mild reaction conditions and is environmentally friendly. The raw materials are cheap and easy to obtain, which provides a new route for synthesizing the antidiabetic drug sitagliptin phosphate.
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