http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105017081-B

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Predicate Object
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D203-20
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C271-22
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C269-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C271-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C269-00
filingDate 2015-07-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2017-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2017-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-105017081-B
titleOfInvention A kind of preparation method of sitagliptin intermediate
abstract The invention discloses a kind of preparation method of sitagliptin intermediate, belong to pharmaceutical synthesis field, the step of this preparation method is (1) ring-opening reaction:In the medium with methyl tertiary butyl ether(MTBE) for the oxolane, temperature is subzero 20 DEG C to subzero 50 DEG C, with Cu-lyt. as catalyst, 2,4,5 trifluorobromobenzenes and grignard reagent RMgX, wherein R is isopropyl, there is grignard reaction for halogen in X, the compound of generation occurs ring-opening reaction with compound as shown in Equation 3 again, obtains compound as shown in Equation 4;(2) oxidation reaction:There is oxidation reaction in compound as shown in Equation 4 and potassium permanganate in medium-acetone, be quenched with reducing agent sodium sulfite, sodium sulfite, neutralization, and methyl tertiary butyl ether(MTBE) extracts, and obtains sitagliptin intermediate.The method low cost, high income, technical maturity, suitable industrialized production.
priorityDate 2015-07-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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