4-(2-Substituted-[1,3]thiazolo[3,2-a]benzimidazol-3-yl)quinazolin-2-amines were prepared by the multi-component reaction of 2,4-dichloroquinazoline, terminal alkynes, secondary amines, and 1H-benzo[d]imidazole-2(3H)-thione in the presence of a palladium窶田opper catalyst. This one-pot process provided an efficient and successful approach for the synthesis of a new thiazolo[3,2-a]benzimidazole linked-quinazoline scaffold with good to high yields.