The Dissertation Submitted To Hebei Normal University For Master Of Science Degree

1,5-benzothiazepine is a kind of compound which has important physiological activities. Some of his derivatives have been used in clinic as antianxiety drug, hypnogenetic and cardiovascular medicine. Therefore, its synthesis, structures and pharmacological activities have attracted wide attentions. But reference suggests, in order to get antibacterial effect, high concentration is necessary.In this thesis, in order to choice better compounds with antibacterial activities we have synthesized two series of new 1, 5-benzothiazepines which haven't been reported and researched their antibacterial activities ? the results show 1 , 5-benzothiazepine with acetyl group or ester group have better antibacterial effect. Our work is benefit for finding their other special functions and producing new active chemical compounds. The thesis contains three procedures.1. 3-Phenylmethylene-2, 4-pentanedione and 2- phenylmethylene -3-oxobutanoic ethyl ester were synthesized from benzaldehyde and acetylacetone or ethyl acetoacetate by knoevenagel condensation reaction. We have researched and improved the conditions of seperation and purification.2. 3-Acetyl-2,4-dihydro-4-methyl-2-(4-nitrylphenyl)-1,5-benzothiazepine and 2,4-dihydro-4-methyl-2-(4-methylphenyl)-l,5-benzothiazepine-3-carboxylic acid ethyl ester were synthesized from o-aminothiophenol and 3-phenylmethylene-2, 4-pentanedione or 2- phenylmethylene -3-oxobutanoic ethyl ester.The structures of these productions were determined by IR, 'H NMR,¹³CNMR, MS and elementary analysis.3. We have researched antibacterial activities of these compounds.lt suggestes that some of these compounds have better antibacterial activities to staphylococcus aureus and fungi,but haven't antibacterial activities to E.coli.Because the absence of drugs against fungi,the research is benefit for finding their other special functions and producing new active chemical compounds.