2-（4-苯基哌嗪）喹啉-3-噁二唑啉衍生物的合成

菜单

摘要迄今为止，含N化合物在杀虫剂、除草剂、杀菌剂领域发挥着很大的作用，我们合成的噁二唑啉衍生物是一类含N化合物，和一些天然产物一样，如生物碱、维生素和抗菌素，有多种药理活性，在医药、农药、涂料、高分子合成材料等方面，有广泛用途，受到了科学家们的广泛关注。苯基哌嗪和喹啉，是很重要的药物中间体，如2-苯基哌嗪是抗抑郁药米氯平的中间体、含有4-苯基哌嗪的左羟丙哌嗪具有镇咳活性，I-CPP对肾上腺有良好的选择性，是新的肾上腺髓质显像放射性药物；喹啉及其衍生物由于其优良的生理活性，近年新型的喹啉类药物也被逐渐开发出来，功能有抗疟、抑菌、杀虫、抗心律失常、抑制肿瘤等等。如氯喹、奎宁、阿莫地喹能抗疟，3-甲基氯喹、阿的平抗丝虫成虫安全有效，布喹那抗癌。通过对这类化合物的性质调查和合成方法的研究，我们把4-苯基哌嗪引入到喹啉类化合物中，再改变相关部位的官能团，希望能获得生理活性更好的目标药物，为合成新药提供更好的原料，提高药物疗效，解决人们身体、生活上的烦恼。44024

本论文分为以下两部分：

第一部分为文献综述部分：

该部分主要是对目标产物：2-（4-苯基哌嗪）喹啉-3-噁二唑啉衍生物，即喹啉类衍生物，其合成前原材料和中间产物的生理活性、药理活性的相关阐述，具体内容还包括各大化合物在国内外的发展状况、合成方法，以及它们在医药、农药、化学等领域的应用价值。还对酯化反应做了相应的知识扩充。

第二部分为实验部分，主要工作如下：

1、氯代喹啉醛的合成

2、三氮唑喹啉醛的合成

3、苯基哌嗪醛的合成

4、新型含喹啉基2-（4-苯基哌嗪）喹啉-3-噁二唑啉衍生物的合成

Up until now ,compounds that contain N element are effective pesticides ,herbicides, bactericides ,etc. We have composed the Evil two oxazoline derivatives ,which contain N. Like most natural compounds(Alkaloid ,Vitamin or Antibiotic),have various pharmacological activities ,and have been implied in medicine ,pesticide, fuel , coating , synthetic polymer materials ,and have drawn scientists’ great attention. Phenyl piperazine and quinoline are important intermediates ,for instance ,2- Phenyl piperazine is intermediate of Mv Lvping ,which is a antidepressant, the Levodropropizine has a 4- Phenyl piperazine can resist coughing ,I-CPP is elective to Adrenal gland, this is a new medicine to the radioactivity of Adrenal medulla. A series of quinolne medicine have been created by relative specialists, functions including anti-malaria, anti-bacteria, anti-secticide, anti-arrhythmia, anti-tumor etc. For example ,Chloroquine, Quinine, Amodiaquine ,they can resist malaria,3-methyl chloroquine and quinacrine is functional to adult worms ,brequinar anti cancer .According to our investigations to the synthetic methods ,we combined 4- Phenyl piperazine and quinoline ,and also change some functional groups , hoping to get more effective targets ,that can offer materials to new products and solve people’s health problems .

This dissertation has two parts :

The first is journals reviewed :

It is to cltarget products: 2-（4- Phenyl piperazine）quinoline-3- Evil two oxazoline derivatives, namely, quinoline derives ,it is claim of the physiological activity and pharmacological activity about original materials and the intermediate product, and details include the development and synthetic methods of foreign countries ,the values of them in medicine ,pesticide and chemistry. Chloro benzoic acid react with ethanol and concentrated sulfuric acid to make chloro benzoyl hydrazine is the esterification reaction, therefore ,the content also includes the esterification reaction’s mechanism and representatives.