http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105017081-B
Outgoing Links
Predicate | Object |
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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 |
Incoming Links
Total number of triples: 103.