Invention Grant
US07795438B2 Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride
有权
1-苄基-4 - [(5,6-二甲氧基-1茚满酮)-2-基]甲基哌啶和盐酸盐的制备方法
- Patent Title: Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride
- Patent Title (中): 1-苄基-4 - [(5,6-二甲氧基-1茚满酮)-2-基]甲基哌啶和盐酸盐的制备方法
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Application No.: US10580908Application Date: 2005-04-27
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Publication No.: US07795438B2Publication Date: 2010-09-14
- Inventor: Akio Imai , Hiroshi Nishimura
- Applicant: Akio Imai , Hiroshi Nishimura
- Applicant Address: JP Tokyo
- Assignee: Eisai R&D Management Co., Ltd
- Current Assignee: Eisai R&D Management Co., Ltd
- Current Assignee Address: JP Tokyo
- Agency: Birch, Stewart, Kolasch & Birch, LLP.
- Priority: JP2004-133277 20040428
- International Application: PCT/JP2005/008028 WO 20050427
- International Announcement: WO2005/105742 WO 20051110
- Main IPC: C07D211/32
- IPC: C07D211/32
![Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride](/abs-image/US/2010/09/14/US07795438B2/abs.jpg.150x150.jpg)
Abstract:
Processes for preparing 1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-yl]methylpiperidine (donepezil), which is useful as an intermediate for medicines, and for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (donepezil hydrochloride), which is useful as a medicine. The process for donepezil hydrochloride production comprises catalytically hydrogenating the compound represented by the structural formula (III) [1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-ylidene]methylpiperidine] with a Raney nickel catalyst under mild conditions and subsequently treating it with hydrochloric acid. Thus, impurities are further diminished. The operations are simple and the process is suitable for industrial production.
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