Functionalization of the 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) core

Bioorg Med Chem Lett. 2008 May 15;18(10):3112-6. doi: 10.1016/j.bmcl.2007.10.103. Epub 2007 Nov 1.

Abstract

The new BODIPY systems 1 and 2 were prepared and then used as substrates to explore S(N)Ar and F-B displacement reactions. Chloride was easily displaced from 1 by a piperidine/ester, methylmagnesium bromide selectively displaced fluoride, and cyanide could attack both sites. System 2 readily added soft nucleophiles to the electrophilic carbon atoms, providing a new method for bioconjugation of BODIPYs to proteins while also introducing a (19)F probe.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boron Compounds / chemistry*
  • Chlorides / chemistry
  • Cyanides / chemistry
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / chemistry*
  • Fluorides / chemistry
  • Magnesium Compounds / chemistry
  • Molecular Probes / chemistry*
  • Molecular Structure
  • Piperidines / chemistry

Substances

  • 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
  • Boron Compounds
  • Chlorides
  • Cyanides
  • Fluorescent Dyes
  • Magnesium Compounds
  • Molecular Probes
  • Piperidines
  • Fluorides