PROCESSES FOR PRODUCING 1-BENZYL-4-[(5,6-DIMETHOXY-1INDANON)-2-YL]METHYLPIPERIDINE AND HYDROCHLORIDE THEREOF

Title:

PROCESSES FOR PRODUCING 1-BENZYL-4-[(5,6-DIMETHOXY-1INDANON)-2-YL]METHYLPIPERIDINE AND HYDROCHLORIDE THEREOF

Document Type and Number:

WIPO Patent Application WO/2005/105742

Kind Code:

A1

Abstract:

Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-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-1indanon)-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.

Inventors:

Imai, Akio (C/O EISAI CO, LTD. Kashima-Cite 22, Oaza Sunayama, Hasaki-mach, Kashima-gun Ibaraki 55, 31402, JP)
Nishimura, Hiroshi (C/O EISAI CO, LTD. Kashima-Cite 22, Oaza Sunayama Hasaki-machi, kashima-gu, Ibaraki 55, 31402, JP)

Application Number:

PCT/JP2005/008028

Publication Date:

November 10, 2005

Filing Date:

April 27, 2005

Export Citation:

Click for automatic bibliography generation Help

Assignee:

Eisai R&D Management Co., Ltd. (6-10, Koishikawa 4-chome Bunkyo-k, Tokyo 88, 11280, JP)
Imai, Akio (C/O EISAI CO, LTD. Kashima-Cite 22, Oaza Sunayama, Hasaki-mach, Kashima-gun Ibaraki 55, 31402, JP)
Nishimura, Hiroshi (C/O EISAI CO, LTD. Kashima-Cite 22, Oaza Sunayama Hasaki-machi, kashima-gu, Ibaraki 55, 31402, JP)

International Classes:

B01J25/02; C07D211/32; (IPC1-7): C07D211/32; B01J25/02

Attorney, Agent or Firm:

Asamura, Kiyoshi (Room 331, New Ohtemachi Bldg. 2-1, Ohtemachi 2-chom, Chiyoda-ku Tokyo 04, 10000, JP)

Download PDF:

View/Download PDF PDF Help

Previous Patent: SUBSTANTIALLY PURE 4-[2-(DI-N-PROPYLAMINO)ETHYL]-2(3H)-INDOLONE HYDROCHLORIDE

Next Patent: HISTAMINE-3 RECEPTOR ANTAGONISTS