【作者】 王晓旋；

【导师】 景欢旺；

【作者基本信息】 兰州大学 ， 物理化学， 2010， 硕士

【摘要】 微波促进有机合成(MAOS)是二十世纪八十年代新兴的有机合成方法,与常规加热法比较,具有反应体系受热均匀,增加分子间的碰撞几率,缩短反应时间,提高产品收率等多种优点。包含咪唑并[2,1-b]噻唑骨架的化合物一直被用作驱虫剂,抗高血压,抗炎症,免疫系统抑制剂,杀菌剂,除草剂,抗肿瘤剂和强心剂等等,是一类具有很广泛的生物活性的物质。本论文主要通过微波合成技术合成一系列咪唑并[2,1-b]噻唑类衍生物。具体结论如下：1.本文将首次利用微波合成技术,在功率为200W,微波作用时间很短的情况下,一步合成具有较高产率的6-芳基咪唑并[2,1-b]噻唑类化合物。2.采用零价钯催化对6-芳基咪唑并[2,1-b]噻唑类化合物进行了Heck偶联反应的研究,发现在微波功率400W下,反应高选择性地在咪唑环的4-位上发生。得到一系列5-取代-6-芳基咪唑并[2,1-b]噻唑类衍生物。而且此类Heck反应进一步证实了含有吸电子取代基的卤代芳烃比其他卤代芳烃更容易进行Heck偶联反应。合成具有简单或复杂官能团的环丙烷衍生物都带有一定的生化性质,包括酶抑制作用,杀虫性,抗真菌性,除草性,抗生素,抗肿瘤性和抗病毒性等。本文第四章考察了EDA与苯乙烯在CO和手性SalenRu(Ⅱ)存在下各种产物的分配比。以及EDA的自聚反应。更多还原

【Abstract】 Microwave irradiation technique has been applicated in organic synthesis since the 20th century eighties. Compared with the classical heating, the microwave technique have many advantages which can make the reaction system heating uniformly, increase the probability of collisions between molecules, reduce the reaction time, and improve the product yield and so on.Imidazo[2,1-b]thiazoles has been used as anthelmintic, antihypertensive, immune system inhibitors, bacteriostatic, herbicide, antitumor, and cardiotonic activity. Imidazo[2,1-b]thiazoles is a class of bioactive substances.This paper syntheses a series of imidazo[2,1-b]thiazoles by microwave irradiation technique. The specific conclusions are listed as followed:1. In the power of 200W, we have synthesized a series of 6-Arylimidazo [2,1-b]thiazoles firstly by microwave irradiation technique, and received higher yield in a short time.2. We have studied the Heck reaction on the 6-Arylimidazo[2,1-b]thiazoles by catalysis of Palladium(0), and obtain a series of 5-Substituted-6-Arylimidazo[2,1-b] thiazoles. In the power of 400W, the Heck reaction has high regioselectivity, and the substrates can bear substitutent in the fourth position in the imidazole ring. And the withdrawing electronic halogenated alkylbenzene can react more easily than other halogenated alkylbenzenes.Occurring and synthetic cyclopropanes bearing simple or complex functionalities are endowed with a large spectrum of biological properties, including enzyme inhibition and insecticidal, antifungal, herbicidal, antibiotic, antitumour, and antiviral activities and so on. In chapter 4, we have studied the reaction between EDA and styrene, in the Chiral catalyst system SalenRu(Ⅱ) and CO. And the EDA’s self-polymerization has also been studied. We can see the distribution ratio of different products.更多还原