A novel synthetic method has been developed with palladium-catalyzed Buchwald-Hartwig-type reaction for the synthesis of N-tert-butyl-3-{[2-(arylamino)pyrimidin-4-yl]amino} benzenesulfonamide 5 by the treatment of N-tert-butyl-3- [(2-chloropyrimidin-4-yl)amino] benzenesulfonamide 4 with different aromatic amines in the presence of Cs 2 CO 3 and in DMF under microwave conditions. All the eight compounds 5a-h were evaluated for their antibacterial, antifungal, and cytotoxic activities. Among the title compounds, 5c and 5d showed potent activity towards both gram-positive and gram-negative bacteria. Compounds 5c and 5d displayed good antifungal activity, and the compounds 5c, 5d, and 5f exhibited significant cytotoxicity activity.