Bifunctional Lewis Base Catalyzed Asymmetric N-Allylic Alkylation of 2-Hydroxypyridines

Org Lett. 2022 Dec 2;24(47):8603-8608. doi: 10.1021/acs.orglett.2c03207. Epub 2022 Nov 20.

Abstract

A chiral Lewis base catalyzed enantioselective N-allylic alkylation of 2-hydroxypyridines and MBH carbonates is documented, affording a convenient access to N-alkylated 2-pyridones with up to 99% ee and 99% yield. Experimental and computational studies have revealed that the strong hydrogen bond interaction between the chiral Lewis base catalyst and 2-hydroxypyridines plays a crucial role in this reaction for the reactivity, chemoselectivity, and enantioselectivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Hydrogen Bonding
  • Lewis Bases*
  • Pyridones*

Substances

  • Lewis Bases
  • 2-hydroxypyridine
  • Pyridones