Iridium-Catalyzed Borylation of 6-Fluoroquinolines: Access to 6-Fluoroquinolones

J Org Chem. 2022 Aug 5;87(15):9977-9987. doi: 10.1021/acs.joc.2c00973. Epub 2022 Jul 15.

Abstract

The Ir-catalyzed C-H borylation of fluoroquinolines has been realized. The quinoline boronic ester formed undergoes a range of important transformations of relevance to medicinal chemistry. Judicious choice of the substituent at C4 on the quinoline facilitated the unmasking of a fluoroquinolone─the core structure of many antibiotics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boron Compounds / chemistry
  • Catalysis
  • Fluoroquinolones*
  • Iridium* / chemistry
  • Molecular Structure

Substances

  • Boron Compounds
  • Fluoroquinolones
  • Iridium