New Synthesis of Donepezil Through Palladium‐Catalyzed Hydrogenation Approach

Abstract

A new, economical, and efficient process has been developed for large‐scale synthesis of donepezil 1, an anti‐Alzheimer's drug. The process involves palladium‐catalyzed hydrogenation of (2E)‐5,6‐dimethoxy‐2‐(pyridin‐4‐ylmethylene)indan‐1‐one 6 to provide 5,6‐dimethoxy‐2‐(piperidin‐4‐ylmethyl)indan‐1‐one 8 as a key step.

DRL‐IPD Communication No. 006.

Keywords:

• Anti‐Alzheimer's drug
• donepezil
• economic synthesis
• palladium‐catalyzed hydrogenation

Acknowledgment

The authors thank management of Dr. Reddy's Laboratories Ltd. for supporting this work. Cooperation from the project colleagues is highly appreciated.

Notes

DRL‐IPD Communication No. 006.