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Predicate Object
classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04
filingDate 2015-10-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2018-06-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2018-06-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-106608876-B
titleOfInvention A kind of preparation method of high-purity palbociclib
abstract The invention relates to a preparation method of high-purity palbociclib. The method is to utilize acetoacetate to reflux and dehydrate under the action of an acid catalyst to prepare 2-acetyl-3-methyl-2-pentaconate diethyl (M) ester (Ⅲ), and then dehydrate it with trimethyl orthoformate Methanol condensation obtains 2-acetyl-3-methyl-4-methoxymethylene-2-pentaconate diethyl (methyl) ester (Ⅳ), and then with N-(5-(4-tert-butoxy Cylcarbonyl-1-hexahydropiperazinyl)-2-pyridyl)guanidine (Ⅴ) obtains 2-acetyl-3-[[5-(4-tert-butoxycarbonylpiperazine-1 ‑yl) pyridin‑2‑yl] amino]‑3H‑4‑ketone‑dihydropyrimidinyl‑2‑butene ethyl (methyl) ester (Ⅵ), and finally compound VI and cyclopentylamine cyclization, de-Boc protecting group Get Paboscini. The raw materials used in the invention are cheap and easy to obtain, the process flow is short, the operation is simple and convenient, the method is environmentally friendly, the reaction selectivity is good, and the product yield and purity are high.
priorityDate 2015-10-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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