Invention Grant
- Patent Title: Process for the manufacture of memantine and intermediate product
- Patent Title (中): 美金刚和中间产品的制造方法
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Application No.: US12736198Application Date: 2009-03-19
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Publication No.: US08436209B2Publication Date: 2013-05-07
- Inventor: Florian Anton Martin Huber , Giorgio Gallo , Carla De Faveri
- Applicant: Florian Anton Martin Huber , Giorgio Gallo , Carla De Faveri
- Applicant Address: DE Frankurt am Main
- Assignee: Merz Pharma GmbH & Co. KGaA
- Current Assignee: Merz Pharma GmbH & Co. KGaA
- Current Assignee Address: DE Frankurt am Main
- Agency: Hueschen and Sage
- Priority: EP08005371 20080320; EP08020340 20081121
- International Application: PCT/EP2009/002049 WO 20090319
- International Announcement: WO2009/115334 WO 20090924
- Main IPC: C07C231/08
- IPC: C07C231/08 ; C07C233/57

Abstract:
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.
Public/Granted literature
- US20110082317A1 PROCESS FOR THE MANUFACTURE OF MEMANTINE AND INTERMEDIATE PRODUCT. Public/Granted day:2011-04-07
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