A series of new 2‐alkyl/arylbenzothiazoles has been synthesized on the basis of the potent and selective in vitro anti‐tumor properties of 2‐(3,4‐diethoxyphenyl)‐5‐fluorobenzothiazole. The synthesis of benzothiazole analogs was achieved via microwave irradiation of a 1:1 mixture of o‐aminothiophenol and alkyl/aryl acylacetonitriles at temperature of 200°C for 10 min. The yields are very good to excellent. All the products were characterized by 1H nmr, 13C nmr and elemental analysis.