In order to obtain potent biological active compounds, a convenient and efficient method for the synthesis of compounds comprising 2‐imino‐2,5‐dihydrofuran, aromatic, sulfamoyl, and heterocyclic fragments has been presented. This environmentally friendly method was based on the reaction of 2‐imino‐2,5‐dihydrofuran‐3‐carboxamides with analgesic and sulfanilamide drugs and 4‐aminoantipyrine in glacial acetic acid and afforded high yields of the products.