Synthesis And Antimicrobial Activity Of3-Ch₂CO₂Et Substituted-2,4-diary-1,5-Benzothiazepine

1,5-Benzothiazepine is a kind of heterocycle compound in clinical, which has importantphysiological activities. Some of its derivatives have been used in clinic as antianxietydrugs,hyprosis and cardiovascular medicines. Therefore, its syntheses, structures andpharmacological activities have been attracted wide attentions.This group has been engaged in the1,5-benzothiazepine research work for a longtime,and got ester substituent Benzothiazepine which has better inhibitory effect in fungal. Atthe sane time, filted derivatives of such characteristics. In order to choice better1,5-benzothiazepine with antibacterial activities, twenty novel3-CH₂COOEt substituted1,5-benzothiazepine derivatives are designed and synthesized then researched in depth. At thesame time, Changed the reaction condition such as solvents or catalysts，then recived the bestreaction conditions,compared the yield with HPLC and Separation production rate.The main jobs in this thesis is as follows:Fristly, through Friedel-Crafts acylation reaction synthesized compounds Ⅱa-g Withbenzene, fluorobenzene, chlorobenzene, bromobenzene, toluene and succinic anhydride as thestarting material. In the polar solvents ethanol, the reaction of substituted benzaldehydes withunsaturated acid under alkaline conditions, and then with thiophenol occurred Michaeladdition reaction and dehydration cyclization reaction synthesised twenty new3-CH₂COOC₂H5-2,4-diary-1,5-benzothiazepine compounds. All the structures of thesecompounds are determined by IR,1HNMR, MS and x-ray single crystal diffraction method.Secondly, Focused on the reaction conditions of synthesis1,5-benzothiazepine, detailworks had been researched. Filter optimum condition from the point of view of solvents andcatalysts, then find the best catalyst cerous chloride and best solvent chloroform.Thirdly, Research the relationship of biological activity test and structure-activity ofⅤa-g andⅥh-t, this work laid a theoretical foundation for exploring new1,5-benzothiazepinecompounds.Fourthly, Cultivated single crystal and determined the structure by single crystaldiffraction...