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2. 发明申请

WO2009115334A2 PROCESS FOR THE MANUFACTURE OF MEMANTINE AND INTERMEDIATE PRODUCT 审中-公开
标题翻译：制造和中间产品的过程
公开(公告)号：WO2009115334A2
公开(公告)日：2009-09-24
申请号：PCT/EP2009002049
申请日：2009-03-19
申请人： MERZ PHARMA GMBH & CO KGAA , HUBER FLORIAN ANTON MARTIN , GALLO GIORGIO , DE FAVERI CARLA
发明人： HUBER FLORIAN ANTON MARTIN , GALLO GIORGIO , DE FAVERI CARLA
IPC分类号： C07C231/08 , C07C233/03
CPC分类号： C07C231/08 , C07C2603/74 , C07C233/03
摘要： The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 5O0C. The present invention also relates to the overall process of manufacturing Memantine from 1,3-dimethyladamantane by means of hydrolyzing the intermediate NFORM.
摘要翻译：本发明涉及N-甲酰基-1-氨基-3,5-二甲基金刚烷的制备方法，该方法是制备1-氨基-3,5-二甲基金刚烷盐酸盐（美金刚）的总体方法中的中间产物。其中，该方法包括以下步骤：（a）使1,3-二甲基金刚烷与包含浓硫酸和浓硝酸的酸混合物反应，其中使用1至6体积份硫酸（以ml计）以重量份计的1,3-二甲基金刚烷（以g计）; （b）使来自步骤（a）的溶液与从步骤（a）中每摩尔脱质子化的1,3-二甲基金刚烷的1至5摩尔当量变化的甲酰胺反应得到N-甲酰基-1-氨基-3,5 -dimethyladamantane。在步骤（b）中，总酸的摩尔比，即硫酸的摩尔量和硝酸的摩尔量相对于甲酰胺的摩尔量的摩尔比为至少1.5，温度为至少50℃。本发明还涉及通过水解中间体NFORM从1,3-二甲基金刚烷制造美金刚的整个方法。

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