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filingDate 2007-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9b5e5fff98cbdd184bfd4004827e8f6e
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_87ea5dec9072a362d5498593ad25229b
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publicationDate 2008-10-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1978014-A1
titleOfInvention Process for the preparation of entacapone and intermediates thereof
abstract New preparation process for the preparation of entacapone which comprises converting the 3,4-dimethoxy-5-nitrobenzoic acid into an activated derivative which is reacted with 2-cyano-N,N-diethylacetamide in the presence of a base to give 2-cyano-3-(3,4-dimethoxy-5-nitrophenyl)- N , N -diethyl-3-hydroxyacrylamide; reacting the resulting compound with MHB(OCOR) 3 where R is (C 1 -C 4 )-alkyl, phenyl, or CF 3 ; and M is a sodium, potassium or ((C 1 -C 4 )-alkyl) 4 N, in the presence of an appropriate solvent to give E -2-cyano-3-3,4-dimethoxy-5-nitrophenyl)- N,N -diethylacrylamide; and finally submitting the compound obtained to a demethylation reaction to yield entacapone. Both 2-cyano-3-(3,4-dimethoxy-5-nitrophenyl)- N,N -diethyl-3-hydroxyacrylamide and E -2-cyano-3-3,4-dimethoxy-5-nitrophenyl)- N,N -diethylacrylamide are new. Entacapone has industrial applicability as antiparkinson's agent.
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http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2251323-A1
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