Abstract A simple and highly efficient methodology for the synthesis of 1, 2, 4, 5-tetrahydro [1] benzothiepino [4, 5-e]-imidazo [1, 2-c] pyrimidine (XI) having a novel ring system via 4- substituted 5, 6-dihydro [1] benzothiepino-[5, 4-d] pyrimidines VII-X is described. The anti- platelet aggregation activity for it and its related compounds against collagen-induced aggregation of rabbit blood platelets in vitro was found.