Construction of a Chiral β-Fluoroamine by Asymmetric Mannich Reaction of 2-Fluoroindanone with Pyrazolinone Ketimines

J Org Chem. 2023 Jun 16;88(12):7736-7747. doi: 10.1021/acs.joc.2c02040. Epub 2023 Feb 7.

Abstract

The asymmetric Mannich reaction of 2-fluoroindanone with ketimine was developed under the catalysis of a kind of chiral copper complex, affording a chiral tetrahedral center containing fluorine. A series of β-fluoroamine derivatives can be obtained in excellent yields (73-94%) with high diastereoselectivities (>99:1 dr) and enantioselectivities (89-99%). The possible transition state was supported by density functional theory calculation.

MeSH terms

  • Catalysis
  • Imines*
  • Nitriles*
  • Stereoisomerism

Substances

  • ketimine
  • Imines
  • Nitriles