http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110003220-B

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-54
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-265
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C51-412
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-265
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C51-41
filingDate 2019-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-01-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2021-01-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-110003220-B
titleOfInvention Preparation method of tofacitinib citrate
abstract The invention discloses citric acidA preparation method of tofacitinib. The method comprises the following steps: 1) carrying out desalting reaction on the compound shown in the formula II under an alkaline condition to obtain an intermediate shown in the formula III; 2) reacting an intermediate shown in a formula III, ethyl cyanoacetate and alkali in an inert atmosphere in the presence of an alkaline ionic liquid to obtain a reaction solution containing tofacitinib alkali; 3) and adding monohydrate citric acid into the reaction solution containing tofacitinib alkali to carry out salt forming reaction to obtain tofacitinib citrate. In the preparation process of the invention, a proper amount of [ Bmim ] is added]Im and a combination of triethylamine and pyridine in a specific ratio is selected as a base, and the ionic liquid is used as a solvent for the reaction on one hand and a catalyst on the other hand, so that the reaction can be promoted to be rapidly carried out, and meanwhile, the yield and the purity of the product are improved.
priorityDate 2019-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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