The Stduy Of Synthesis And Relevant Reaction Of 1,5- Benzothiazepine And It's Derivatives

1,5-benzothiazepine is a kind of compound which has important physiological activities. Some of its derivatives have been used in clinic as antianxiety drugs, hyprosis and cardiovascular medicines.Therefore, its syntheses, structures and pharmacological activities have been attracted wide attentions. Experiments proved that 1,5– benzothiazepine are a class of compounds with specific structures. Through the antibacterial activity of the compounds,We have found that different structures of these compounds have different physiological activity.At present, the research group for the Synthesis of research work mainly focused on the synthesis of 1,5 - benzothiazepine-β-lactam and 1,5 - benzothiazepine these two types of compounds. We have analyzed antibacterial activity of all the various compounds that have been synthesized.It is the consequent that with ester of 1,5- benzo-N-imine-type heteropoly compounds Zhuo has good antibacterial activity. Our preliminary view is that ester and imine double bond are the efficacy of such compounds, functional groups. In order to clarify imine double bond is the efficacy of such compounds that is one functional group. In this paper Selective reduction methods of containing ester and double bond in the imine of 1,5 - benzo-N-imine-type heteropoly compounds Zhuo were studied. Its antimicrobial activity of1,5 - benzothiazepine derivatives will be very good if its mother ring 2 C atoms are replaced by ester. Therefore, in this thesis long chainα,β-unsaturated ketones synthetic methods are carried out relevant research. The job provides an important theoretical basis for studing of synthesis with a special pharmacological activity of 1,5 - benzothiazepine class of drugs.The main jobs in this thesis is as follows:Fristly, In this paper Selective reduction methods of containing ester and double bond in the imine of 1,5 - benzo-N-imine-type heteropoly compounds Zhuo were studied. And the experimental conditions were optimized for the work..Secondly, using the above reduction method, We successfully synthesizedⅣa-e of these five compounds. And We determine their structuresthrough the characterization work..Thirdly,Ⅳa-e these five compounds were determined in vitro antifungal activity of work. Measurement results show that the antibacterial activity ofⅣcompounds significantly decreased (Ⅲcompounds with antimicrobial activity in comparison). Therefore, we can clearly see that imine double bond is ond kind of important antibacterial functional group of these compounds.Fourthly, in this paper we have studied the imine, enamine-type 1,5 - benzothiazepine the configuration transformation of the conditions .And we have arrived at a certain separation of the isomers of the best experimental conditions.Fifthly, in the paper we have designed long chainα,β-unsaturated ketones of the synthetic route. Some of the experimental conditions of synthesis ofγ-and right pairs of F-phenyl-α,β-unsaturated enone ester E (ie F chalcone) were optimized. The work provides an experimental basis for the synthesis of novel 1,5 - benzothiazepine Zhuoyan biological research.