Synthesis Of α-maleamic Group-β-lactam Derivatives Of Dihydro-1,5-benzothiazepine And The Search Of Their Antimicrobial Activities

1,5-benzothiazepines are a kind of compounds with important biological activities, such as treating for neural and heart diseases. Their structures, syntheses and pharmacological activities have attracted wide attention in recent years. Benzothiazepines can be modified or derived from the C=N double bond where chemical reactions occurred. Thus a series of new 1,5-benzothiazepine derivatives have been synthesized and developed.In order to developβ-lactam ntibiotics compounds with new biological activities, the paper introduces the [2+2] cycloaddition reaction which take place between 1,5-benzothiazepines and acylchloride, and preparesα-maleamic group-β-Lactam derivatives of 1,5-benzothiaepines. Their stereoche-stry and reaction mechanisms have been investigated in detail. The main research results are as follows:1. We synthesize a series ofα-maleamic group-β-Lactam derivatives of 1,5-benzothiaepines. The synthesis procedure is glycine through the following steps such as–NH₂ protection, -COOH activation, and then reacting with benzothiazepine. The chemical structures are determined by 1H NMR, MS, IR and Elementary Analysis.2. In order to study the seletive stereo-chemistry reaction between 1,5-benzothiazepines and ketenes, the stereo-structure of the products are analysed by X-ray diffraction .3. We have researched antibacterial activities of these compounds through the method of filter paper. The results indicate that these compounds have the antibacterial activities.