Friday, February 20, 2015


Common name: Donepezil; Aricept; Domepezil; E2020; E 2020; Donepezil hydrochloride
Trademarks:  Aricept; Alzepil; Donecept; Donepex
Molecular Formula: C24H29NO3
CAS Registry Number: 120014-06-4
CAS Name: 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
Molecular Weight: 379.492
InChI: InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3
Activity: Reversible Acetylcholinesterase Inhibitor;  Alzheimer's disease Treatment; AD Treatment; Severe Dementia Therapy
Status: Launched 1996
Originator: Eisai Pharma/Pfizer

Donepezil synthesis: EP296560 (also Ref. 2)

Donepezil synthesis: Org Process Res Dev 2008, 12(4), 731-735
Donepezil synthesis: WO1999036405A1

Donepezil synthesis: Synth Commun 200636, 169-174

1. Sugimoto, H.; et. al. EP296560
2. Sugimoto, H.; et. al. Synthesis and Structure-Activity Relationships of Acetylcholinesterase Inhibitors: 1-Benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine Hydrochloride and Related Compounds. J Med Chem 1995, 38(24), 4821-4829.
3. Mathad, V. T.; et. al. An Improved and Efficient Process for the Production of Donepezil Hydrochloride: Substitution of Sodium Hydroxide for n-Butyl Lithium via Phase Transfer Catalysis. Org Process Res Dev 2008, 12(4), 731-735.
4. Limura, Y. Process for production of donepezil derivative. WO1999036405A1
5. Elati, C.; et. al. New Synthesis of Donepezil Through Palladium-Catalyzed Hydrogenation Approach. Synth Commun 2006, 36, 169-174.
6. Dooley, M.; et. al. Donepezil: a review of its use in Alzheimer's disease. Drugs Aging 2000, 16(3), 199-226. (activity)
7. Birks, J. S.; et. al. Donepezil for dementia due to Alzheimer's disease. Cochrane Database Syst Rev 2003, (3), CD001190. (activity)
8. Malouf, R.; et. al. Donepezil for vascular cognitive impairment. Cochrane Database Syst Rev 2004, (1), CD004395. (activity)