Efficient and Industrially Viable Synthesis of Donepezil |
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Authors: | R Janaki Rama Rao Y L N Murthy |
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Institution: | 1. Natco Research Centre, Natco Pharma Limited , Hyderabad, Andhra Pradesh, India;2. Department of Organic Chemistry , Andhra University , Visakhapatnam, Andhra Pradesh, India |
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Abstract: | An efficient, economically viable process has been developed for large‐scale preparation of donepezil HCl (1), an anti‐Alzheimer's agent. The process involves the condensation of 5,6‐dimethoxy‐1‐indanone (3) and 1‐benzyl‐4‐piperidinecarboxaldehyde (4) in the presence of alkalimetal carbonates at elevated temperature to yield 1‐benzyl‐4‐(5,6‐dimethoxy‐1‐indanone)‐2‐yidenyl] methyl piperidine (2), the key intermediate in the synthesis of donepezil. Hydrogenation of 2 yields donepezil. |
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Keywords: | anti‐Alzheimer's agent aqueous alkali metal carbonates condensation donepezil economically viable |
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