Synthesis of phosphorylated isoindolinone derivatives

Abstract The synthesis of diethyl [2-(2-alkyl-3-oxo-2,3-dihydro-1 H -isoindol-1-yl)ethyl]phosphonates and diethyl [3-(2-alkyl-3-oxo-2,3-dihydro-1 H -isoindol-1-yl)propyl]phosphonates, via metallation ( sec -BuLi) of N-substituted isoindolin-1-ones and then the reaction of the generated lithiated species 4 with diethyl vinylphosphonate or diethyl 3-bromopropylphosphonate, respectively, is described.