Process for preparation of donepezil

Details Process for preparation of donepezil Process for preparation of donepezil

2006-12-12

2006-12-12

Chang, Celia (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S205000, C546S238000, C546S324000

Reexamination Certificate

active

07148354

ABSTRACT:
An efficient process for preparation of donepezil is provided. In one embodiment, the process for preparation of donepezil includes suspending a catalyst, which is palladium metal on carbon and the compound of the structurein an alcoholic solvent and hydrogenating the suspension at the hydrogen pressure of from about 1 to about 5 and a temperature of from about 40 to about 90° C. till the hydrogenation reaction is substantially complete to obtain a compound of the formula (VI):which then converted to donepezil. The processes of the invention are believed to be simple, eco-friendly, and commercially viable.

REFERENCES:
patent: 4895841 (1990-01-01), Sugimoto et al.
patent: 5606064 (1997-02-01), Lensky
patent: 6649765 (2003-11-01), Vidyadhar et al.
patent: WO 97/22584 (1997-06-01), None
Sugimoto et al. Shnthesis and anti-acetylcholinesterase . . . Bioorg. Med. Chem. Let. v. 2 *8) p. 871-876 (1992).
Sam et al. “Reduction products . . . ” J. Het. Chem. v.2 (4) p. 366-370 (1965).
Exhibit A search result for making formula VI.

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