Studies On The Synthesis And Antimicrobial Activity Of2-carbalkoxyalkyl/n-propyl-1,5-benzothiazepines

With the improvement of people’s living standard，the medical cause rapid development,benzothiazepines compounds have wide application. Benzothiazepines cause the concentration ofthe researchers because of the important biological activity.1,5-benzozepine is a kind of very important benzothiazepines compounds, we ResearchGroup have been concentrating in the field,and have find some benzozepines which havegood antibaterial effect. On that basis, we research the chain growth of the benzozepine’ lateralchain and the change of the bacteriostatic activity of the benzozepine, and discuss the structureactivity relationship. This thesis includes the major parts:1.We make γ–butyrolactone and methanol for raw materia,after ester exchange reaction,the product is Oxidized to4-Oxo-butanoic acid methyl ester by ShaRui special reagent， and4-Oxo-butyric acid ethyl ester is synthetized with the similar method. This reaction was studied.2. Acetophenone and Br2are used for the creation reaction of1-bromination-acetophenone,and wittig reagent is created. Wittig reagent and4-Oxo-butanoic acid methyl ester go to run thereaction to get6-aryl-6-Oxo-4-methyl caproate, furthermore, the reagent and2-amino benzenesulfur phenol go to run the reaction to create seven new2-CH₂CH₂COOCH₃substituted1,5-benzothiazepines and three2-CH₂CH₂COOC₂H₅substituted1,5-benzothiazepines.Thestructures of all the compounds were established by IR、1H NMR、MS and elemental analysis.Wealso studied about the mechanism and condition of various reaction deeply.3.We use wittig reagent and n-butanal to generate fourteen new2-CH2CH2CH3substituted1,5-benzothiazepines,and the structures of all the compounds were established by IR、1H NMR、MS and elemental analysis. We studied about part of the reaction.4. We test the bacteriostatic activity of the twenty-four new benzothiazepines.5. We study some kinds of method to create6-Ar-6-Oxo-4-hexenoicacid methyl ester.