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A process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine of the formula I:c r Formula I commonly known as lamotrigine which comprises :a) reduction of 2,3'dichloronitrobenzene of the formula IX Formula IX in Ci -Ce aliphatic alkanol with hydrogen at a pressure of 55-90 psi in the presence of a metal catalyst at 27 - 35°C;b) diazotisation of the resulting 2,3-dichloroaniline of the formulaX Formula X with sodium nitrite and a mineral acid at -5° to 5'''C followed by cyano-de-diazonation with a metal cyanide at 65 - 80°C, c) hydrolysis of the resulting 2.^-dichlorobenzonitrile ofthe formulaXI : c-ChJ Formula XIunder acidic or alkaline conditions;d) chlorination of the resulting 2,3-dichlorobenzoic acid of the formula VI: with a chlorinating agent at 55 - 130°C, e) cyano-de-halogenation of the resulting 2,3-dichloro-benzoyl chloride of the formula VII ;CcclFormula VII with a metal cyanide in the presence of an alkali metal iodide by refluxing in an aproticsolvent under an inert atmosphere;f) condensation of the resulting 2,3-dichlorobenzovlcyanide of the formula VIII: f . :ccbiFormula VIIIwith aminoguanidine bicarbonate in an organic solvent in acidic conditions in the presence of a catalyst at 90° - 125°C followed by insitu cyclisation of the resulting Schiff s base of the formula IV : Formula IV by refluxing in an aliphatic alkanol in the presence of a base; and g) purification of the resulting crude lamotrigine of the formula I:c1Formula I by a known method such as recrystalhsation from an aliphatic alkanol or chromatographic separation.
Notices, Deadlines & Correspondence
Patent Information
Applicants
RPG LIFE SCIENCES LIMITED
Inventors
1. RADHAKRISHNAN TARUR
2. SASIKUMAR THOOVARA MOHAN
3. SRIVASTAVA ANITA RANJAN
Specification
Documents
Application Documents
| # | Name | Date |
|---|---|---|
| 1 | in-pct-2002-00829-mum-power of attorney(23-3-2004).pdf | 2018-08-08 |
| 2 | IN-PCT-2002-00829-MUM-PATENT CERTIFICATE-(13-1-2006).pdf | 2018-08-08 |
| 3 | in-pct-2002-00829-mum-form-pct-isa-210(3-12-2003).pdf | 2018-08-08 |
| 4 | in-pct-2002-00829-mum-form-pct-ipea-409(3-12-2003).pdf | 2018-08-08 |
| 5 | in-pct-2002-00829-mum-form 3(17-6-2002).pdf | 2018-08-08 |
| 6 | in-pct-2002-00829-mum-form 3(12-1-2004).pdf | 2018-08-08 |
| 7 | in-pct-2002-00829-mum-form 26(17-6-2002).pdf | 2018-08-08 |
| 8 | in-pct-2002-00829-mum-form 2(granted)-(31-8-2004).pdf | 2018-08-08 |
| 10 | in-pct-2002-00829-mum-form 1a(19-6-2002).pdf | 2018-08-08 |
| 11 | in-pct-2002-00829-mum-form 19(19-8-2003).pdf | 2018-08-08 |
| 12 | in-pct-2002-00829-mum-form 19(13-8-2003).pdf | 2018-08-08 |
| 13 | in-pct-2002-00829-mum-correspondence(ipo)-(17-8-2004).pdf | 2018-08-08 |
| 14 | IN-PCT-2002-00829-MUM-CORRESPONDENCE(IPO)-(17-3-2006).pdf | 2018-08-08 |
| 15 | in-pct-2002-00829-mum-correspondence(5-8-2004).pdf | 2018-08-08 |
| 16 | in-pct-2002-00829-mum-claims(granted)-(31-8-2004).pdf | 2018-08-08 |
| 18 | in-pct-2002-00829-mum-cancelled pages(31-8-2004).pdf | 2018-08-08 |