The amination of difluoro(diethoxyphosphoryl)acetyl chloride: Facile synthetic route to novel amides containing difluoromethylenephosphonate moiety

A convenient route for the synthesis of novel amides containing at least one β-keto-α,α-difluoromethylenephosphonate group has been elaborated. The procedure requires simple stirring of an amine and difluoro(diethoxyphosphoryl)acetyl chloride in THF in the presence of a catalytic amount of DMAP. A wide range of amines has been accepted, including aliphatic and aromatic diamines, diaminobenzidine or amine derivatives, such as Ciprofloxacin.