A new commercially viable synthetic route for donepezil hydrochloride: anti-Alzheimer's drug.
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 overall yield of the process.
Dubey
Shailendra Kumar
SK
Chemical and Pharma Research Department, Jubilant Organosys Limited, Cairo 11562, Egypt.
Kharbanda
Manita
M
Dubey
Sushil Kumar
SK
Mathela
Chandra Shekhar
CS
D000544:Alzheimer Disease / Q000188:drug therapy; D000077265:Donepezil; D006801:Humans; D007189:Indans / Q000138:chemical synthesis*; D018697:Nootropic Agents / Q000138:chemical synthesis*; D010880:Piperidines / Q000138:chemical synthesis*; D013678:Technology, Pharmaceutical / Q000191:economics / Q000379:methods*
D007189:Indans; D018697:Nootropic Agents; D010880:Piperidines; D000077265:Donepezil