Process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine, commonly known as lamotrigine
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United States of America Patent
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Oct 28, 2003
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N/A
app pub date -
Jun 24, 2002
filing date -
Jan 3, 2000
priority date (Note) -
Expired
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Abstract
A process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3-5-diamine (lamotrigine) of the formula I: ##STR1## 2,3-Dichloronitrobenzene in C.sub.1 -C.sub.6 aliphatic alkanol is hydrogenated at 55-90 psi gas pressure using metal catalyst at 27-35.degree. C. 2,3-Dichloroaniline is diazotised and cyano-de-diazonised with metal cyanide at 65-80.degree. C. 2,3-Dichlorobenzonitrile is hydrolysed and 2,3-dichlorobenzoic acid is chlorinated at 55-130.degree. 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.degree. 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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