Synthesis 2022; 54(23): 5253-5260
DOI: 10.1055/a-1894-8826
paper

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

Authors

  • Sen Wang

  • Rui Miao

  • Yanping Xia

  • Yifei Wei

  • Renshi Luo

  • Lu Ouyang


The National Natural Science Foundation of China (22161003), and Gannan Medical University (QD201810, TD2021YX05) are acknowledged for financial support.


Graphical Abstract

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.

Supporting Information



Publication History

Received: 20 April 2022

Accepted after revision: 08 July 2022

Accepted Manuscript online:
08 July 2022

Article published online:
15 August 2022

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