Synthesis And Antimicrobial Activity Of 2-CO₂Et Substituted -1,5-Benzoxazepine And Study On Ester Exchange Reaction Of γ-Butyrolactone With Alcohols

1,5-benzothiazepine is a kind of compound which has important physiological activities. Some of its derivatives have been used in clinic as antianxiety drug, hyprosis and cardiovascular medicine. Therefore, its syntheses, structures and pharmacological activities have been attracted wide attentions. But reference suggests, in order to get antibacterial effect, high concentration is necessary. In order to choice better 1,5-benzothiazepine with antibacterial activities, we have designed and synthesized seven novel 2-alkoxyl carbonyl-4-aryl-1,5-benzoxazepines. The structures of the productions were determined by IR, 1H NMR,MS and elementary analysis. meanwhile, the productions were researched about their antibacterial activities. This thesis ofγ-butyrolactone ester exchange reaction in-depth research, and to further optimize the reaction.This thesis includes there major parts:1.This paper is chosen maleic anhydride and benzene derivatives,by Friedel-Crafts acylation reaction synthesis ofⅠa-g, then esterification with ethanol synthesis ofⅡa-g, then, in polar solvents and acidic conditions with 2-amino-phenol synthesis of new and seven novel 2-alkoxyl carbonyl-4-aryl-1,5-benzoxazepines. And optimize each step, each step has been the best reaction conditions. The thesis of the new compounds synthesized by IR,1HNMR, MS and elemental analysis, determination, and then use the measured spectra of these new compounds were characterized. the synthesis of these new compounds were antifungal testing laboratories. Studied the antibacterial activity of these compounds structure-activity relationship. This work found to have more good for the inhibitory effect of the new oxygen azepine compounds provide an experimental basis.2.In-depth study and exploration of theγ-butyrolactone ester exchange reaction, namely temperature and time on the major factorsγ-butyrolactone ester exchange reaction, optimization of the reaction. Study of the strong acid ion exchange resin adsorption and reuse. After the work on the transesterification of lactones to provide experimental basis.