Synthesis Of New [1,5]benzothiazepine Derivatives Containing 2-Phenyl-1,2,3-triazole

The 1,5-benzothiazepines are a kind of seven-membered ring heterocyclic compounds which possess many physiological properties. They are often used as tranquilizer and medicines for cardiovascular disease. Scientist shown great ardor in it's synthesis, structure, and physiological properties research. In previous literatures, the research of 2-heterocycle substituted 1,5-benzothiazepines is seldom. Therefore, we expect to realize reinforcement of many physiological activities by introduction of 2-phenyl-1,2,3-triazole ring into 1,5-benzothiazepine, and obtained a series of new compounds with stronger biological activities. In addition we combined 1,2,4-oxodiazole which has strong biological activities with 1,5-benzothiazepines by 1,3-dipolar cycoladdition reaction respectively, and a series of derivatives with novel structures were synthesized. Besides, we have discovered a new methods to synthesize some new benzothiazole.The thesis includes two major parts:The first part is about literature review:The important synthetic methods, structure and chemical transformation of 1,5-benzothiazepine derivatives that have been studied in China and other countries were explicated systematically and briefly elucidated 1,2,3-triazole ring.The second part is about experimental content. Major work as follows:1. Syntheses of 3-(2-phenyl-1,2,3-triazole-4-yl)-5-Aryl-4,5-Dihydro Pyrazole Derivatives.α,β-unsaturatedketon synthesized from 2-phenyl-4-acetyl-1,2,3-triazole and a series of right-Substituted benzaldehydes, which reacted with phenylhydrazine under refluxing to give pyrazoline derivatives.2. Synthesis of New 1,5-benzothiazepines Containing 2-Phenyl-1,2,3-triazole. 1,5-Benzothiazepines containing 2-phenyl-1,2,3-triazole which have potentially useful pharmacological properties were synthesized fromα,β-unsaturated ketones and 2-aminothiophenol .3. Synthesis of New 1,2,4-Oxadiazolo[5,4-d][1,5]benzothiazepine Derivatives Containing 2-Phenyl-1,2,3-triazole 1,5-benzothiazepine under went 1,3-dipolar cycloaddition reaction with aryl nitrile oxides"insitu"and a seres of 1,2,4-oxadiazolo-[5,4-d][1,5]benzothiazepine derivatives containing 2-phenyl-1,2,3-triazole were obtained.4. Synthesis of New 2,6-di(2-phenyl-1,2,3-triazolo-4-yl)-3-Substituted phenyl-3H,4H-pyridine [2,1-b]Benzothiazole 1,3-di(2-phenyl-4-acetyl-1,2,3-triazolo-4-yl)-2-right-Substituted phenyl propane synthesized from 2-phenyl-4-acetyl-1,2,3-triazole and a series of right-substituted benzaldehydes, which reacted with 2-aminothiophenol under refluxing and a series of new Benzothiazole derivatives were obtained. Above all, the structures of the new compounds were confirmed by elememtal analysis, IR, 1H NMR and MS spectral data, and discussed it's spectral property. We give single crystal discussion to part of these compoundes.