Cu catalyzed [4 + 2] cycloaddition for the synthesis of highly substituted 3-fluoropyridines

Org Biomol Chem. 2022 May 11;20(18):3731-3736. doi: 10.1039/d2ob00133k.

Abstract

A copper catalyzed annulation-aromatization of benzyl trifluoromethyl ketimines with 3-acryloyloxazolidin-2-ones for the synthesis of 3-fluoropyridines through double C-F bond cleavages has been developed. In this approach, the annulation occurred between the in situ formed dienes from trifluoromethyl ketimines via the first C-F bond cleavage and 3-acryloyloxazolidin-2-ones. Then the aromatization afforded 3-fluoropyridines in moderate yields through the second C-F bond cleavage. The 3-fluoropyridine products could be further hydrolyzed to multi-substituted 3-pyridinecarboxylic acids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Copper* / chemistry
  • Cycloaddition Reaction
  • Molecular Structure

Substances

  • Copper