Ir-Catalyzed α-Alkylation of Ketones with Alcohols: One-Step Access to Donepezil

Abstract

We demonstrate an iridium-catalyzed alkylation of ketones with alcohols, which enables one-step access to donepezil, including cyclic ketones and linear ketones in high yields. Scale-up experiment exhibits the excellent practicability of this protocol. Comparative experiments show that a small amount of water is beneficial to the improvement of product yield.