The Synthesis Of 1, 5-Benzothiazepine And Pyrazoline Derivatives Containing Pyrazole

Heterocyclic compounds play an important role in the fields of medical and pesticides.It has been a hot topic to synthesize heterocyclic compounds containing bioactivities and pharmalogical activities by human synthsis in medical chemistry and pesticide chemistry. In fact, the works greatly contribute to human's healthy and development of agriculture. The works go on in view of these observation and expect to realize the inforcement of many physiological activities by means of combining different heterocycles to one moleculer.Pyrazole nitrogen-containing heterocycles is intensively applied in pharmaceutical and agrochemical industries due to their antipyretic, anti-inflammatory,herbicidal, insecticidal and fungicidal properties. In the beginning of this century, Somebody began to synthesize the compoud, then, many chemists develop lots of pyrazole derivatives containing more activities by introducing new substituent or combining the pyrazole heterocycle to other heterocycles, which also have good activities.1,5-benzothiazepine and 1,2,4-oxadiazole heterocycles exhibit diverse biological activities. Of the two heterocycles, 1,5-benzothiazepine compounds have been used as anticonvulsants and tranquilizer drugs and drugs for cardiovascular disease. 1,2,4-oxadiazole also have attracted wide-spread attention due to their potent activities such as antiviral fungicide and anti-inflammatory. In the papers, I combine the aboved three heterocycles to one moleculer and synthesize a series of new heterocycles with a various structure by designing different synthetic procedures. the structures of intermediate and target compounds were estiblished by elemental analysis, 1H NMR, IR data.The detail works in the paper:1. 1-phenyl-3-methyl-5-aryloxyl-pyrazol-4-carboxaldehyde reacted with acetophenone or para-substituted acetophenones to formα,β-unsaturated ketone by condensation reaction And the reaction of theα,β-unsaturated ketone with 2-amino thiophenol gave 1,5-benzothiazepines containing 1-phenyl-3-methyl-5-aryloxyl-pyrazole.2. 1,5-benzothiazepine synthesized underwent 1,3-dipolar cycloadditon reaction with aryl nitrile oxides″in situ″and a series of 1,2,4-oxadiazolo[4,5-d][1,5]benzothiazepine derivatives containing 1-phenyl-3-methyl-5- aryloxyl-pyrazol were obtained.3. New pyrazoline deriravatives containing pyrazole have been synthesized whileα,β-unsaturated ketone containing 1- phenyl- 3- methyl- 5- aryloxyl- pyrazol react with hydrazine hydrate and phenyl hydrazine in glacial acetic acid under refluxing...