Synthesis of α-Fluorinated Phosphonates from α-Fluorovinylphosphonates: A New Route to Analogues of Lysophosphatidic Acid

Abstract
A versatile, efficient method for the preparation of α-monofluoromethylene (−CHF−) phosphonates from α-fluorovinylphosphonate provides access to a class of lysophosphatidic acid (LPA) receptor-subtype agonists. In addition, sn-2 O-methylation of α-monofluoromethylene phosphonates using trimethylsilyldiazomethane generated sn-1-acyl, 2-O-methyl α-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 α-monofluoromethylene LPA analogues was prepared.