A New Commercially Viable Synthetic Route for Donepezil Hydrochloride: Anti-Alzheimer's Drug

…, M Kharbanda, SK Dubey, CS Mathela

Index: Dubey, Shailendra Kumar; Kharbanda, Manita; Dubey, Sushil Kumar; Mathela, Chandra Shekhar Chemical and Pharmaceutical Bulletin, 2010 , vol. 58, # 9 p. 1157 - 1160

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Citation Number: 5

Abstract

An economical new process has been developed for the synthesis of donepezil hydrochloride (1) an anti-Alzheimer's drug. The process involves Darzen reaction of pyridine- 4-carboxaldehyde and 2-bromo-5, 6-dimethoxy indanone affording epoxide 5, 6-dimethoxy- 3-(pyridine-4-yl) spiro [indene-2, 2′-oxiran]-1 (3H)-one (4) as a key intermediate. The one- pot deoxygenation of 4 and hydrogenation of the aryl moiety in high yield improved the ...