含1,2,4三唑环的芳氧吡啶甲酰胺的合成与研究.doc

含1,2,4三唑环的芳氧吡啶甲酰胺的合成与研究
摘要
杂环化合物在农药的发展中发挥了十分重要的作用,尤其是含氮杂环化合物,具有很高的生物活性,被广泛应用于农药和医药科研中,长期以来,一直是化学工作者研究的热点。含氮杂环化合物中含有吡啶环、嘧啶环的化合物活性高,用途尤为广泛。此外,稠杂环新农药的研究与开发己成为21世纪世界农药发展的主流方向。为了探寻新型多活性中心含氮杂环农药,并实现其活性叠加,增大杀菌、除草谱和提高植物生长调节活性效果,本文合成了3种新型多活性中心含氮杂环酰胺类化合物,结构经IR分析所确证。
本文选择含氮杂环化合物作为研究的目标,主要进行了以下两个方面研究内容:
第一部分: 本文通过检索文献,对二芳醚类、酰胺类、三唑类及含吡啶类化合物的生物活性及发展趋势作了初步的阐述。文中先以2-氯烟酸和苯酚为原料,经过醚化、酸化合成新型中间体化合物2-芳氧基烟酸,实验中探讨了合成芳氧基烟酸的合成路线,并对其最佳碱用量配比、原料配比、反应时间、反应温度、溶剂的种类选择及用量和升温速率的影响进行研究,取得了初步的成果。
第二部分:以三种不同取代基的苯甲酸为原料,合成了三种含1,2,4三唑环的稠杂环胺类化合物。利用生物等排体原理,通过亚结构连接法,本实验从2-芳氧基烟酸出发,经酰氯化,再与三种胺类化合物进行酰胺化反应,得到含1,2,4-三唑环的酰胺类目标化合物,这三种新型酰胺均未见文献报道。
采用红外光谱、对目标化合物进行了结构表征,并对其物理化学性质、波谱性质、反应条件、合成方法进行了分析和探讨。目标化合物(II1~II3)的结构式如下:
III1:

III2:

III3:
关键词:合成;杂环化合物;芳氧吡啶;三唑;酰胺
Synthesis and Studies on phenoxy-poundsIncluding 1,2,4- triazole ring
Abstract
pounds playing an in creasingly important role in the developentment of pesticide, especially nitrogen pounds. Multi-activity centered nitrogen pounds have good activities in pesticide and medicine fields. They have been researched as hot-topic area for a long time. the activities are high among nitrogen pounds which include pyridine. In order to find novel multi-activity centered nitrogen heterocyclic pesticides and realize the accumulation of activities,enlargement of herbicide and fungicide spectra, enhancement of plant growth regulation activity, 3 new multi-activity centered nitrogen pounds were synthesized. Their structures have been confirmed by IR.
The article set nitrogen pounds as goals of research. The thesis includes mainly two aspects:
Part one:This article by retrieving a document, on ethers species, amide species, triazole and class and pyridine derivatives . Using 2-chloro Nicotinic Acid and phenol as raw materials , the article synthesized late-model intermediate product 2-aryloxy Nicotinic Acid by etherification、acidification. Furthermore, the article researched synthetic route、the optimal dosage of alkali、the ratio of material、the reactio