http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109651459-B

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Predicate Object
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H15-18
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H15-18
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H1-00
filingDate 2019-01-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-09-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-09-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-109651459-B
titleOfInvention Preparation method of gemcitabine intermediate methanesulfonyl ester
abstract The invention relates to a preparation method of gemcitabine intermediate mesyl ester, belonging to the technical field of synthesis of drug intermediates. In order to solve the problems of low conversion rate and large waste liquid amount of the existing method, the method for preparing gemcitabine intermediate mesyl ester comprises the steps of carrying out reduction reaction on 2-deoxy-2, 2-difluoro-D-erythro-1-furanose-3, 5-dibenzoyl ester of a compound shown in a formula I in a mixed solvent of a water-insoluble organic solvent and catalytic amount of isopropanol to convert the compound into a compound shown in a formula II; and cooling the temperature of the reaction solution to control the temperature of the reaction solution to be below 5 ℃, and adding methylsulfonyl chloride to perform esterification reaction to obtain the corresponding gemcitabine intermediate methylsulfonyl ester of the compound shown in the formula III. The method can effectively improve the reaction speed and the conversion rate, reduce the generation of impurities, has higher yield and purity requirements, can realize the one-pot reaction, and simplifies the production operation.
priorityDate 2019-01-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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