Coumarin Derivatives, Synthesis And Antibacterial Activity Was Detected

Coumarin is a kind of important organic chemical raw material and intermediate, which can be widely used as medicines, pesticides, spicery products, and other chemical industries.The coumarin derivatives were synthysized from 7-hydroxycoumarin by the Williamson etherification reaction and fluorination. Their biological activity were investigated in this thesis.Many factors which affected the etherification reaction, such as ratio of batching, reaction temperature, catalyst and reaction time had been studied. Optimum conditions of synthesis of 7-(2,2,2-trifluoroethoxy) coumarin were obtained as follows: the volume of 7-hydroxycoumarin, TsOCH₂CF₃, NMP and NaOH were 1.62g(10mmol), 4.06g (16mmol) ,10mL respectively, reacting 4h under 200℃. The yield was 88%. Optimum conditions of synthesis of 7-methoxycoumarin were obtained as follows: the volume of 7-hydroxycoumarin, Me₂SO₄, K₂CO₃ and acetone were 0.81g(5mmol), 0.94mL(10mmol), 1.24g(9mmol), 30mL respectively, reacting 8h under refluxing temperature. The yield was 90%.