铜催化喹啉类衍生物磺酸酯化反应的研究
Abstract: On the basic study of the preparation route of quinoline N- oxide, an effective synthetic route to quinoline derivatives via copper-catalyzed sulfonic acid esterification was explored in this paper as well as . Optimization Studies was conducted and the scope of the reaction was investigated.
This method used facile quinolones and 3-chloroperbenzoic acid to prepare one of the substrate quinoline N-oxides, then reacted with sulfonyl chloride in mild conditions and copper catalysis, various bioactive sulfonic acid esterified quinolone products that would be difficult to synthesize by other methods were obtained in good yields. The reaction shows an excellent tolerance to a number of functional groups and the operation is simple and mild with inexpensive as the. This new reaction allows the preparation of valuable products a more effective synthetic route with high atom economy and promotes green chemistry. Meanwhile, it also expands applications of copper-based catalysts in synthetic and catalytic research fields.
Moreover, we study the application of reaction product in the synthesis of pharmaceutically active substances and explore products, medical value.
毕业论文关键词：N-喹啉氧化物； 铜催化； 磺酸酯化； 绿色化学；
Keyword: quinoline N-oxides; copper-based catalysts; sulfonic acid esterification; green chemistry
目录
1 引言 4
1.1喹啉类衍生物的磺酸酯化反应的研究背景 4
1.2 喹啉类衍生物的磺酸酯化反应的最新研究进展 5
1.2.1过渡金属催化喹啉环C-H选择性功能化 5
1.2.2 N-喹啉氧化物的合成与应用 14
1.2.3 N-喹啉氧化物与磺酰氯的C-H活化反应 14
1.3 未来研究方向 17
1.4 选题意义 17
2 实验部分 17
2.1实验仪器及试剂 17
2.2 铜催化合成喹啉磺酸酯类化合物反应的探究及条件的优化 19
2.2.1反应的初步探究 19
2.2.2溶剂的筛选 20
2.2.3碱的筛选 21
2.2.4催化剂的筛选 22
2.2.5其他反应条件的筛选 23
2.3 反应的底物适应性研究 24
2.3.1 普适性探究实验的方案、步骤及技术路线 24
2.3.2 结果与讨论 25
3结论 35
参考文献 35
致谢 37
1 引言
1.1喹啉类衍生物的磺酸酯化反应的研究背景
随着社会的发展，科技的进步，人们对生活质量和生命意识日益提高，喹啉及喹啉类衍生物在很多自然产品、生物活性化合物和功能材料中有着广泛的应用前景。例如在医药工业，许多喹啉化合物都是重要医药中间体，很多都具有杀菌、抗菌、抗高血压、抗过敏、抗肿瘤和抗癌等药理活性，[1]而且近年来许多含喹啉环的新型药物被不断开发出来，其制备及应用受到人们的高度关注，具有良好市场前景。典型的例子是喹啉磺酸酯类衍生物拥有有良好的医药生物活性。
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