Synthesis And Antimicrobial Activities Of New1,5-Benzothiazepines

1,5-benzothiazepines is a kind of good physiological and pharmacological activities of heterocyclic compound,therefore they are widely used in medical and health field,this kind of compounds in the treatment of cardiovascular disease,mental illness,antibacterial,etc,have remarkable curative effect,said that in recent years has been wide attention and research.Our laboratory engaged in 1,5-benzothiazepines and antibacterial activity of the research,create multiple series of 1,5-benzothiazepines,some of the 1,5-benzothiazepines have very high antibacterial activity.1,2,4-triazole because of its itself has good antibacterial activity,are widely used in the field of medical and health care,introducing thiazole ring 1,2,4-triazole and 1,5-benzothiazepines,superposing the reactive group,will significantly affect the compound antibacterial activity,the work on the graduate student has been tried,this thesis is on the basis of previous work,to amend,supplement and perfect.The main content of this thesis:(1)with different substituent benzene as raw material,after Friedel-Crafts acylation,alpha bromine generation reaction,nucleophilic substitution reaction of three azole nitrogen,mannich reaction,Michael addition reaction and other steps to get a 3-(1,4-trichlorobenzene triazole)-4-instead of phenyl 1,5-benzothiazepines.(2)with different substituent benzene as raw material,after fu-grams of acyl reaction,mannich reaction,Michael addition reaction steps of a new class of 4-instead of phenyl-1,5-benzothiazepines.(3)by 1 HNMR,13 CNMR and MS,IR and elemental analysis of target compounds structure characterization.(4)on each step reaction were studied,discussed the mechanism of the byproduct produced.(5)test the in antimicrobial activity,and carries on preliminary structure-activity relationship study.