http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-106045969-B

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Predicate Object
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04
filingDate 2016-05-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2019-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2019-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-106045969-B
titleOfInvention A kind of synthetic method of the card than replacing Buddhist nun
abstract A kind of synthetic method the invention discloses card than replacing Buddhist nun.(R)-N-Boc-2- carboxylic acid piperidin is successively carried out salt-forming reaction and bromination reaction with silver nitrate (or mercury oxide), bromine water by this method respectively;Obtained (R)-N-Boc-2- bromine piperidines is first reacted with magnesium rod and generates Grignard Reagent, then carries out grignard reaction with 1- benzyloxycarbonyl group azetidine -3- ketone;Obtained 1- benzyloxycarbonyl group -3- hydroxyl -3- [(2S)-N-Boc-2- piperidyl]-azetidine is subjected to deamination protection reaction;Obtained 3- hydroxyl -3- [(2S)-N-Boc-2- piperidyl]-azetidine and 2,3,4- trifluorobenzoyl chloride are subjected to amidation process;Obtained [2,3,4- trifluorophenyl] [3- hydroxyl -3- (2S)-N-Boc-2- piperidyl -1- azelidinyl] ketone and the fluoro- 4- Iodoaniline of 2- are subjected to substitution reaction, deamination protection reaction is finally carried out, obtains card than for Buddhist nun.The process route of this method is rationally succinct, and operation simplifies, and it is a kind of environmentally protective method that cost is relatively low, is suitable for industrialized production.
priorityDate 2016-05-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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