http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2003088094-A1
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-14 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 |
filingDate | 2002-10-30^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_be4e7f4c8dba8aa909a60918f6b35612 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c457cf046a14c0e6538a7a527a8fa046 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9129c515ad173b16c5821029fcfb68f6 |
publicationDate | 2003-05-08^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | US-2003088094-A1 |
titleOfInvention | Novel synthesis and crystallization of piperazine ring-containing compounds |
abstract | The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C. The method of the present invention also includes reacting 2-amino-3-hydroxymethyl pyridine with N-methyl-1-phenyl-2,2′-iminodiethyl chloride to form 1-(3-hydroxymethylpyridyl-2)-4-methyl-2-phenyl piperazine, and adding sulfuric acid to the 1-(3-hydroxymethylpyridyl-2)-phenyl-4-methylpiperazine to form mirtazapine. The present invention also relates to new processes for recrystallization of mirtazapine from crude mirtazapine. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2006008302-A3 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2006008302-A2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2008207896-A1 |
priorityDate | 1999-04-19^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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