http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-104447445-B
Outgoing Links
Predicate | Object |
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classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C315-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C317-28 |
filingDate | 2014-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2016-07-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2016-07-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-104447445-B |
titleOfInvention | A kind of preparation method of synthetic Apremilast intermediate |
abstract | The invention relates to a preparation method for synthesizing an intermediate of apremilast. The method utilizes 3-ethoxy-4-methoxy-benzoic acid ester and dimethyl sulfone to generate 2-(3-ethoxy-4-methoxyphenyl) base through condensation reaction under alkaline conditions. -1-Methanesulfonyl ethyl ketone (II); the compound II reacts with chiral amine in the presence of an acidic catalyst to obtain 1-N-substituted amino-1-(3-ethoxy-4-methoxy)phenyl -2-Methanesulfonylethylene (Ⅲ), the obtained compound III is directly hydrogenated in the presence of a hydrogenation catalyst without separation to obtain the product (S)-1-(3-ethoxy-4-methoxy)phenyl- 2-Methylsulfonylethylamine (I), which is the intermediate of Apremilast, can also be further made into N-acetylamino L-leucine salt. The invention also provides a preparation method of apremilast. The technical process of the invention is simple, safe and environment-friendly, low in cost and beneficial to clean industrialized production. |
priorityDate | 2014-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 89.