http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103319399-B

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Predicate Object
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B57-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-02
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-56
filingDate 2013-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2016-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2016-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-103319399-B
titleOfInvention The preparation method of Egelieting intermediate R-3-amino piperidine dihydrochloride
abstract A kind of method that the main object of the present invention is to provide that route is brief, environmental protection, low cost prepare SYR-322 intermediate R 3 amino piperidine dihydrochloride.Reaction uses raceme compound 3 piperidine formamide cheap and easy to get as raw material, under 1 fluoronaphthalene, the hydrogen peroxide effect with fluoboric acid, the Hoffmann rearrangement reaction of similar amide occurs, obtains 3 amino piperidines of fewer than substrate carbon number 1.This reaction condition is simple, can carry out under room temperature;During simple to operate, it is easy to monitoring;Solvent for use is ethanol water mixture, cheap, environmental protection.Contracting carbon product 3 amino piperidine is acidified into salt through concentrated hydrochloric acid, and gained hydrochlorate, after the fractionation of D tartaric acid, becoming salt, obtains the double hydrochloric acid of target product R 3 amino piperidine, and chiral purity is high, and ee value is more than 99.5%.Reaction gross production rate is up to 89% 93%, and cost is relatively low, is especially suitable for industrialized great production.
priorityDate 2013-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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