Synthesis and in vivo evaluation of 4-deoxy-4,4-difluoro-KRN7000

Org Lett. 2008 Oct 16;10(20):4433-6. doi: 10.1021/ol801663m. Epub 2008 Sep 18.

Abstract

The synthesis of 4-deoxy-4,4-difluoro-KRN7000 starting from phytosphingosine is described. Key steps include a regioselective benzylation of azidophytosphingosine and a deoxofluor-mediated fluorination of the corresponding 4-ketone. This fluorination failed completely when the adjacent 3-OH was protected as benzyl ether but proceeded well when a benzoyl group was used. The biological evaluation reveals a bias toward Th1 cytokine induction upon Natural Killer T cell activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzene / chemistry
  • Cytokines / metabolism
  • Galactosylceramides / chemical synthesis*
  • Galactosylceramides / chemistry
  • Galactosylceramides / pharmacology*
  • Killer Cells, Natural / drug effects
  • Killer Cells, Natural / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Molecular Structure

Substances

  • 4-deoxy-4,4-difluoro-KRN7000
  • Cytokines
  • Galactosylceramides
  • Benzene
  • KRN 7000