A novel four-step methodology for the synthesis of 5-acyl-1, 2-dihydropyrimidin-2-ones has been developed. The reaction of readily available N-[(1-acetoxy-2, 2, 2-trichloro) ethyl] ureas with Na-enolates of 1, 3-diketones or β-oxoesters followed by heterocyclization–dehydration of the oxoalkylureas formed gave 5-acyl-4-trichloromethyl-1, 2, 3, 4-tetrahydropyrimidin-2- ones. The latter, in the presence of NaH, eliminate CHCl3 to give the target compounds.
