Synthesis of 2,4-substituted-1,5-substituted-benzothiazepine was carried out. First step was synthesis 1-(4-bromo-1-hydroxynaphthalen-2-yl)ethanone by the acetylation of 4-bromo-alphanapthol in presence of glacial acetic acid and zinc chloride. In the second step 1-(4-bromo-1-hydroxynaphthalen-2- yl)-3-aryl-prop-2-en-1-one obtained by treating 1-(4-bromo-1-hydroxynaphthalen-2-yl) ethanone with aromatic aldehydes using ethanol as a solvent and 40% KOH. The synthesized compound on microwave irradiation in presence of substituted aminobenzenethiol and zinc acetate gave titled benzothiazepine derivatives. The synthesized compounds are characterized by elemental analysis, 1H NMR, IR Spectroscopy. Newly synthesized compound were also studied for their biological activities.