Synthesis And Antimicrobial Activities Of 3- Substituted Benzoyl/4- Substituted Phenyl Of 1,5-benzothiazepines

1,5-benzothiazepines are a kind of seven-membered heterocycle compounds and have important physiological activity, many of these compounds have been used in clinic as antipsychotic drugs, cardiovascular agents etc. So for a long time, studied the 1,5-benzothiazepine structure modification and physiologically active have been received extensive attention by researchers.Our laboratory there has long been engaged in the synthesis of 1,5-benzothiazepine derivatives and the research of their antimicrobial activity, we have synthesized several series of 1,5-benzothiazepine compounds. The 1,5-benzothiazepine derivatives of 3-1,2,4- triazole substituted in the seven-membered heterocycle, have carried out the in vitro tests of antimicrobial activity, and the results indicated it has high antimicrobial activity. In accordance with the principle of added or reduced the carbon chain can improve the efficacy of lead compounds. On the basis of our laboratory preliminary work, designed and synthesised of 1,2,4-triazole methylene substituted 1,5-benzothiazepine compound by add a carbon in the seven-membered 3 site, and compared the antimicrobial activity. During the experiment, in which two-step reaction did not get the desired product, accidentally got two types novel and unreported of structure, 3- substituted benzoyl / 4- substituted phenyl-1, 5-benzothiazepine.The main job in this thesis is as follows:Firstly, two types novel and unreported of structure, 3- substituted benzoyl/4- substituted phenyl-1,5-benzothiazepine was synthesized by the Friedel-Crafts acylation reaction, Mannich reaction, addition elimination reaction ect six steps reaction, which different substituted benzene was used for the raw materials.Secondly, the characterization of target product structure by 1H NMR、13C NMR、MS、 IR and elemental determine.Thirdly, respectively, a detailed study each step of reaction conditions, the main product and by-products formation process and influence factors were discussed in this paper.Lastly, test the antimicrobial activity of the target product.