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1. 发明申请

US20050203287A1 Process for the preparation of sulfamate derivatives 审中-公开
标题翻译：制备氨基磺酸酯衍生物的方法
公开(公告)号：US20050203287A1
公开(公告)日：2005-09-15
申请号：US11077722
申请日：2005-03-11
申请人： Chandrasekhar Batchu , Biju Kumar Pillai , Shekhar Bhirud
发明人： Chandrasekhar Batchu , Biju Kumar Pillai , Shekhar Bhirud
IPC分类号： C07D317/44 , C07H5/06
CPC分类号： C07H9/04 , C07D317/44 , C07H11/00
摘要： An improved process for the preparation of sulfamate derivatives such as topiramate is provided comprising (a) reacting an alcohol with sulfuryl chloride in the presence of an amine base and in a first halogenated hydrocarbon solvent selected from the group consisting of aliphatic halogenated hydrocarbon solvents having 1 to 12 carbon atoms and at least three halogen atoms, aliphatic halogenated hydrocarbon solvents having 2 to 12 carbon atoms and less than three halogen atoms, aromatic halogenated hydrocarbon solvents having 6 to 18 carbon atoms and mixtures thereof to produce a chlorosulfate intermediate and (b) reacting the chlorosulfate intermediate with an amine of the formula R1NH2, wherein R1 is hydrogen or an alkyl from 1 to 4 carbon atoms, in a second halogenated hydrocarbon solvent selected from the group consisting of aliphatic halogenated hydrocarbon solvents having 1 to 12 carbon atoms and at least three halogen atoms, aliphatic halogenated hydrocarbon solvents having 2 to 12 carbon atoms and less than three halogen atoms, aromatic halogenated hydrocarbon solvents having 6 to 18 carbon atoms and mixtures thereof.
摘要翻译：提供了一种制备氨基磺酸酯衍生物如托吡酯的改进方法，其包括（a）在胺碱存在下使醇与磺酰氯反应，并且在选自脂族卤代烃溶剂的第一卤代烃溶剂中具有1 至12个碳原子和至少三个卤素原子，具有2至12个碳原子和少于3个卤素原子的脂族卤代烃溶剂，具有6至18个碳原子的芳族卤代烃溶剂及其混合物，以产生氯代硫酸盐中间体和（b）使氯代硫酸盐中间体与式R 1 NH 2的胺反应，其中R 1是氢或1至4个碳原子的烷基在选自具有1至12个碳原子和至少3个卤素原子的脂族卤代烃溶剂的第二卤代烃溶剂中，脂族卤代具有2至12个碳原子和少于3个卤素原子的烃溶剂，具有6至18个碳原子的芳族卤代烃溶剂及其混合物。

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