- 學位論文
以微波加熱輔助合成具生化活性之雜環分子衍生物
Microwave-assisted synthesis of biologically active heterocyclic molecule derivative
摘要
許多重要的生理物質包括diazepines、thiazepines、oxazepines、benzimidazoles和benzothiazoles，及其類似結構之衍生物。這些分子的生物活性，例如血清素衍生物執行多種生理功能，作用於中樞和外週神經系統多樣性的受體亞型，廣泛分佈於有機體中； 5- HT受體亞型的一些拮抗劑 (如ondansetron 或granisetron) 對於預防和治療嘔吐與抗癌具有很高的療效；這類化合物另一個治療應用，是用來調節腸胃蠕動。因此這一系列的芳香族雜環化合物之衍生物就引起有機化學家的廣泛興趣，並研究其合成方法及生化活性。 我們應用微波輔助開發一個新的並且有效率的合成方法，來合成具生物活性的七元環並帶有兩個雜原子之雜環化合物。（例如，1,4-benzothiazepines、1,4-benzoxazepines、benzimidazoles 和 benzothiazoles) 。 小分子的雜環結構，往往是發生活性的主要地方。 根據上述的研究，變化其取代基，利用微波催化能很快的合成所需的活性化合物及其衍生物。
並列摘要
Many important physiological materials comprise benzimidazoles、benzoxazoles、benzothiazoles、diazepines、 thiazepines and oxazepines or relative structures, for example serotonin derivatives fulfill multiple physiological roles in both the central and peripheral nervous system by acting on a diversity of receptor subtypes widely distributed in the organism. Some antagonists of this 5-HT receptor subtype (e.g., ondansetron or granisetron) are of high therapeutic interest in the prevention and treatment of vomiting associated with anticancer chemotherapy. Another therapeutic use suggested for this class of compounds is regulation of gastrointestinal motility. Our target was the synthesis of new compounds possessing 7-membered rings with two heteroatoms of 1,4-thiazepines. Recently the attention has been concentrated on the synthesis of analogs having additional fused ring. Since heteroaromatic derivatives of benzimidazole have received intense attention, several members of this series have been prepared through different synthetic routes. We have been interested in developing new, more efficient, and synthetically useful reactions for the synthesis of biologically active molecules under microwave -assisted. We describe herein a novel and efficient synthesis of a series of heteroaromatic derivatives. (e.g., 1,4-benzothiazepines、1,4-benzooxazepines、benzimidazoles and benzothiazoles) The heterocyclic structure of small molecules is a place where an activity occurs，This structure changes the nucleophiles and substituent.According to this study, active compound and their derivative can be composed through the Microwave-assisted method. Keywords: 1,4-benzothiazepines microwave–assisted synthesis heterocyclic structure