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, cyclic ketones, and linear ketones in high yields. A scale-up experiment shows the excellent practicability of this protocol. Comparative experiments show that a small amount of water is beneficial to the improvement of product yield.