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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-075
filingDate 2000-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2003-10-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_65547b89590f04ceba9fd0c08a582f45
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15fd74cd723918a95f5a97c428e6fcea
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publicationDate 2003-10-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-6639072-B1
titleOfInvention Process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine, commonly known as lamotrigine
abstract A process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3-5-diamine (lamotrigine) of the formula I:2,3-Dichloronitrobenzene in C1-C6 aliphatic alkanol is hydrogenated at 55-90 psi gas pressure using metal catalyst at 27-35° C. 2,3-Dichloroaniline is diazotised and cyano-de-diazonised with metal cyanide at 65-80° C. 2,3-Dichlorobenzonitrile is hydrolysed and 2,3-dichlorobenzoic acid is chlorinated at 55-130° C. Cyano-de-halogenation of 2,3-dichlorobenzoyl chloride is carried out with a metal cyanide and alkali metal iodide by refluxing in an aprotic solvent under an inert atmosphere. 2,3-Dichlorobenzoyl cyanide is condensed with aminoguanidine bicarbonate in an organic solvent in acidic conditions using catalyst at 90-125° C. followed by insitu cyclisation of the Schiff's base by refluxing in an aliphatic alkanol with base. Crude lamotrigine is purified.
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