http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-106316998-B
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-79 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-79 |
filingDate | 2016-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2019-01-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2019-01-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-106316998-B |
titleOfInvention | A kind of preparation method of prucalopride intermediate |
abstract | The invention belongs to medical synthesis field more particularly to a kind of methods for preparing prucalopride intermediate.This method under suitable acylating agent and lewis acid effect, 0-20 DEG C of temperature control, occurs acylated and demethylating reaction, obtains intermediate (II) specifically includes the following steps: with 2- methoxyl group -4- acetylaminohydroxyphenylarsonic acid 5- chloro benzoic ether (I) for starting material;To alkaline reagent is added in obtained intermediate (II), 0-20 DEG C of temperature control in polar solvent occurs cyclization reaction, obtains intermediate (III);Hydrazine hydrate and dehydrated alcohol are added in intermediate (III), 70-80 DEG C of temperature control, reduction reaction occurs, obtains intermediate (IV);Intermediate (IV) is under sodium hydroxide solution effect, 90-100 DEG C of temperature control, hydrolysis occurs, obtains the sodium salt of intermediate (V), and then be acidified with hydrochloric acid, obtains intermediate (IV).The synthetic route reaction condition is mild, lower production costs, and yield is higher, is suitble to industrialized production. |
priorityDate | 2016-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 64.