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Method for producing memantine and intermediate product
专利权人:
メルツ・ファルマ・ゲーエムベーハー・ウント・コ・カーゲーアーアー
发明人:
フロリアン・アントン・マルティン・フーバー,ジョルジョ・ガッロ,カルラ・デ・ファヴェリ
申请号:
JP2011500120
公开号:
JP5499016B2
申请日:
2009.03.19
申请国别(地区):
JP
年份:
2014
代理人:
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 50° C. The present invention also relates to the overall process of manufacturing Memantine from 1,3-dimethyladamantane by means of hydrolyzing the intermediate NFORM.
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