http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-090100-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ae10212794160b34478f0d05b6ab6fd7 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C313-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C317-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C315-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C317-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B53-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C315-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C317-08 |
filingDate | 2013-02-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2014-10-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-090100-A1 |
titleOfInvention | PROCESSES FOR THE PREPARATION OF (S) -1- (3-ETOXI-4-METOXIFENIL) -2-METHANOSULPHONILETILAMINE |
abstract | Processes for the preparation of intermediate aminosulfone compounds for the synthesis of 2- [1- (3-ethoxy-4-methoxyphenyl) -2-methylsulfonylethyl] -4-acetylaminoisoindolin-1,3-dione, which is useful for prevention or treatment of diseases or conditions related to an abnormally high level of activity of tumor necrosis factor a (TNF-a). In addition, processes for the commercial production of (S) -1- (3-ethoxy-4-methoxyphenyl) -2-methanesulfonylethylamine. Claim 1: A process for the preparation of a compound of formula (1) or a pharmaceutically acceptable salt, hydrate, solvate or polymorph thereof, wherein: R is -CH (C₁₋₆ alkyl) Ar or a hydrogen; R¹ is C₁₋₆ alkyl; R², R³, R⁴, R⁵ and R⁶ are each independently hydrogen, halo, C₁₋₆ alkyl, C₁₋₆ alkoxy, -CF₃, -CN or -NO₂; and Ar is aryl, characterized in that it comprises: (a) the coupling of a benzonitrile optionally substituted with a dialkylsulfone; (b) hydrolysis of the coupled product to produce a b-ketosulfone; (c) the reaction of b-ketosulfone with a chiral auxiliary to form a chiral enamine; (d) reduction of chiral enamine to produce an N-protected aminosulfone; and (e) optionally deprotection of the N-protected aminosulfone. |
priorityDate | 2012-02-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 47.