3 6位取代及n杂环多环类哒嗪衍生物的合成 word格式.docxVIP

摘要哒嗪类衍生物种类多种多样，因其良好的生物活性在农药、医药领域均有 广泛应用，该类衍生物制成的生物药物制剂具有低毒、高效、低残留等特点， 完全符合时下绿色化学及环境友好要求。据相关文献报道可知，其中 3,6-位取代 及向哒嗪类衍生物引入杂原子等因其高效的生物活性成为当今研究热点。本文 从三方面对该类衍生物进行研究分析。1、通过引入不同活性基团对哒嗪环 3,6-位进行取代，从而合成出 3,6-二咪 唑哒嗪、3-氯-6-四氢吡咯哒嗪、3-氯-6-吗啡啉哒嗪，并对其进行相关表征；2、以哒嗪 3-酮类为基体，引入不同活性基团进行取代，合成 6-四氢吡咯哒 嗪-3-甲酸甲酯、6-吗啡啉哒嗪-3-甲酸甲酯，并对其进行相关表征。此外，对 6- 氧代哒嗪-3-甲酸的进行了晶型研究，得到一手性晶型。3、向哒嗪环引入杂原子并成环得到新型 N 杂环多环类哒嗪衍生物，合成 3- 氯-6-肼基哒嗪、3-氯-6-(3,5-二甲基-1H-吡唑-1-基)哒嗪、3-氯-6-(3,5-二苯基-1H- 吡唑-1-基)哒嗪、3-氯-6-(3-乙氧基-5-甲基-1H-吡唑基)哒嗪，并对其进行相关表 征。关键词：哒嗪类衍生物；生物活性；3,6-位取代；多晶型；杂原子；多环IABSTRACTPyridazine derivatives have various species, because its good biological activity is widely used in pesticide, medicine field. Bio-pharmaceutical preparations made by pyridazine derivatives have the characteristics of low toxicity, high efficiency and low residue features, completely conformed to the trial green chemistry and environmental -friendly requirements. According to the relevant literature, 3,6-the introduction of hetero atoms substituted pyridazine derivatives and the efficiency of its biological activity has become the heated research today. In this paper, we will analyze such derivatives through three sides.By introducing different reactive groups on the pyridazine ring of 3,6- substitution position, we got 3,6-di(1H-imidazol-1-yl)pyridazine, 3-chloro-6-(pyrroli din-1-yl)pyridazine , 4-(6-chloropyridazin-3-yl)morpholine, and did some analysis.In pyridazine 3-ones of the matrix, introducing different reactive groups, we got methyl 6-(pyrrolidin-1-yl)pyridazine-3-carboxylate, and did some analysis.Then we did some polymorphs research about 6-oxo-pyridazine-3-carboxylic acid, got a chiral polymorphs.Introducing into pyridazine ring heteroatom and loop to get new pyridazine derivatives, we got 3-chloro-6-hydrazinyl-1H-pyridazine, 3-chloro-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine,3-chloro-6-(3,5-diphenyl-1H-pyrazol-1-yl)pyridazine,3- chloro-6(3-ethoxy-5-methyl-1H-pyrazol-1-yl)pyridazine, and we also did some analys