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A NOVEL PROCESS FOR THE SYNTHESIS OF LAMOTRIGINE AND ITS INTERMEDIATE

机译:拉莫三嗪及其中间体的合成新工艺

摘要

This invention discloses a process for the preparation of 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of a formula (I), commonly known as Lamotrigine which comprises the step of reacting aminoguanidine bicarbonarte and 2,3- dichlorobenzocynide with a reagent prepared by dissolving phosphorus pentoxide and methane sulfonic acid, to produce a novel intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)-acetonitrile monomesylate which is further cyclized to lamotrigine without basification.
机译:本发明公开了通常称为拉莫三嗪的式(I)的3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪的制备方法,该方法包括使氨基胍反应的步骤。用溶解五氧化二磷和甲烷磺酸制得的试剂制备碳酸氢盐和2,3-二氯苯并乙炔生成新的中间体2-(2,3-二氯苯基)-2-(氨基胍)-乙腈单甲磺酸酯,将其进一步环化成拉莫三嗪碱化。

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