Synthesisof-α-group-β-lactam Derivatives Of 1,5-benzothiazepine And The Search Of Their Antimicrobial Activities

1,5-benzothiazepine is a kind of compound with important physiological activities.Their syntheses, structures and pharmacological activities have attracted wide attentions. The C=N double bond in the molecules can modify the benzothiazepine which is one of the major parts where chemical reactions occurred.Thus a series of new 1,5-benzothiazepine derivatives have been synthesized and developed. In order to develop thiazepine compounds with new biological activities , extensive studies on 1,5-benzothiaepine compounds have been done by our group , based on their pesticidal , sterihization and imflammation activities, which can take place [2+2] pericyclic reaction with varies acylchloride to prepareβ-lactam derivaties of 1,5-benzothiaepine.Their spectroscopy character, stereoche-stry and the antibacterial activities have been studied.The main research works are as follows:1 . Two series ofα-succinimide (phhalimide )-β-lactam derivatives of 1,5-benzothiaepines have been synthesized . The synthesis procedure is Glycine through the following steps such as–NH2 protection, -COOH activation, then reacting with benzothiazepine.The chemical structures of the production are determined by 1H NMR, MS, IR and elementary analysis.2.Through pericyclic reaction of 1,5-benzothiaepine and chloroacetyl chloride a series ofα- chloride -β- Lactam derivatives of 1,5-benzothiaepines have been synthesized. The chemical structures of the production are determined by 1H NMR, MS, IR and elementary analysis.3 . In order to study the seletive stereo - chemistry reaction between 1,5-benzothiazepines and acylchloride ,the stereo-structure of the products are analyzed by X-ray diffraction.4.Antibacterial activities of these compounds have been studied through the methods of filter paper.