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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-56
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filingDate 2016-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_60734f64f6f8cbc5434d9df947dbdb60
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_094accbb96653235e802e4bfb3350f97
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publicationDate 2016-12-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-106187887-A
titleOfInvention The preparation method of 4 hydroxyquinoline 3 formic acid
abstract The present invention relates to organic synthesis and the preparing technical field of crude drug intermediate, it is specifically related to the cystic fibrosis therapies new drug preparation method according to key intermediate 4 hydroxyquinoline 3 formic acid cutting down Kato, comprise the steps: (1) condensation reaction: with o-Carboxynitrobenzene, potassium ethyl malonate salt, N, N carbonyl dimidazoles is raw material, and reaction prepares 3 (2 nitrobenzophenone) 3 oxopropanoate;(2) reduction reaction: 3 (2 nitrobenzophenone) 3 oxopropanoate prepare 3 (2 aminophenyl) 3 oxopropanoate through catalytic hydrogen reduction;(3) ring-closure reaction: 3 (2 aminophenyl) 3 oxopropanoate and N, N Dimethylformamide dimethyl acetal, obtains 4 hydroxyquinoline 3 Ethyl formates through nucleophilic addition, ring-closure reaction;(4) hydrolysis: 4 hydroxyquinoline 3 Ethyl formates, through hydrolysis, obtain 4 hydroxyquinoline 3 formic acid.This synthetic route raw material is easy to get, reaction condition gentle, post processing is simple and convenient, is suitable for amplifying preparation, and yield is high.
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priorityDate 2016-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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