- A new approach to the synthesis of lamotrigine and other 3,5-diamino-1,2,4-triazine derivatives
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A new in principle method for the synthesis of 6-aryl(hetaryl)-3,5-diamino- 1,2,4-triazines by decomposition of pre-synthesized tetrazolo[1,5-b][1,2,4] triazines was developed. The advantages of this method over traditional methods were demonstrated using the synthesis of a modern antiepileptic preparation lamotrigine, as an example.
- Ulomskii,Shestakova,Deev,Rusinov,Chupakhin
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p. 726 - 732
(2007/10/03)
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- Process for preparing substituted benzoyl cyanide amidinohydrazones
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The present invention provides a process for preparing a compound of the general formula (I): wherein R1 to R5 are independently selected from hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 alkoxy, all optionally substituted by one or more of halogen, hydroxy and aryl groups, as well as being independently selected from amino, mono- or disubstituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups, which process comprises reacting a compound of the general formula (II): wherein R1 to R5 are as defined in formula (I), with aminoguanidine bicarbonate in a mixture of a water-soluble solvent and polyphosphoric acid.
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- Process for preparing substituted Benzoyl Cyanide Amidinohydrazones
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The present invention provides a process for preparing a compound of the general formula (I):wherein R1to R5are independently selected from hydrogen, halogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl or C1-6alkoxy, all optionally substituted by one or more of halogen, hydroxy and aryl groups, as well as being independently selected from amino, mono- or disubstituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups, which process comprises reacting a compound of the general formula (II):wherein R1to R5are as defined in formula (I), with aminoguanidine bicarbonate in a mixture of a water-soluble solvent and polyphosphoric acid.
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