Synthesis of alpha-fluorinated phosphonates from alpha-fluorovinylphosphonates: a new route to analogues of lysophosphatidic acid

Org Lett. 2003 Jun 26;5(13):2267-70. doi: 10.1021/ol034597+.

Abstract

A versatile, efficient method for the preparation of alpha-monofluoromethylene (-CHF-) phosphonates from alpha-fluorovinylphosphonate provides access to a class of lysophosphatidic acid (LPA) receptor-subtype agonists. In addition, sn-2 O-methylation of alpha-monofluoromethylene phosphonates using trimethylsilyldiazomethane generated sn-1-acyl, 2-O-methyl alpha-monofluoromethylene derivatives. Finally, a novel method for the selective etherification of 1,2-diols was developed and a new class of sn-1 O-methyl, 2-acyl alpha-monofluoromethylene LPA analogues was prepared. [reaction: see text]

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Hydrocarbons, Fluorinated / chemical synthesis
  • Hydrocarbons, Fluorinated / chemistry*
  • Lysophospholipids / chemical synthesis*
  • Lysophospholipids / chemistry*
  • Methylation
  • Organophosphonates / chemical synthesis
  • Organophosphonates / chemistry*
  • Vinyl Compounds / chemistry*

Substances

  • Hydrocarbons, Fluorinated
  • Lysophospholipids
  • Organophosphonates
  • Vinyl Compounds