Abstarct: In this work facile synthesis of new derivatives of imidazo[1,2-a]pyrimidines through palladium-catalyzed heteroannulation is reported. Treatment of 2-aminopyrimidine (4) with propargyl bromide (94) in refluxing acetonitrile affords 2-amino-1-(2-propynyl) pyrimidinium bromide (91) in good yield. When compound (91) was treated in DMF with the aryl halides (92a-g) and triethylamine in the presence of bis(triphenylphosphine)palladium chloride (II) and copper iodide at 70 ºC, the 2-arylsubstituted imidazo[1,2-a]pyrimidines (93a-g) were obtained in good to high yields. The reactions had to be carried out under an argon atmosphere, and the mixture of DMF and triethylamine had to be degassed prior to use.