Abstract
The synthesis of imidazo[1, 5-a]pyrimidines from 2-substituted pyrimidin-4(3H)-ones is described. 2-[(Acylamino)methyl]-6-methylpyrimidin-4-(3H)-ones, prepared by the reaction of β-aminocrotonamide with N-acylated amino acid esters, were treated with POCl3 to give 2- and 4-chloroimidazo[1, 5-a]pyrimidines, which reacted with various nucleophiles to afford 2- and 4-substituted imidazo[1, 5-a]pyrimidines.