摘要：肿瘤的治疗一直是一个世界性的难题，一直困扰着人们的身体健康，所以一直以来备受关注。随着世界的医疗卫生知识的不断普及和现代医疗技术的发展，针对于潜在的新型抗肿瘤先导化合物的研究也越来越受到关注。这类新型的靶向型抗肿瘤药物不断在变化和研究过程中，为未来肿瘤的治疗提供了新的方向，而且加上现在晶体衍射技术、组合化学、分子模型等技术的发展，更加推动了这类药物的发展。4-苯胺喹唑啉衍生物是一类高效的杂环化合物，在抗菌、抗肿瘤、抗病毒等方面都表现出了良好的生物活性，其中一类靶向型抗肿瘤药物就是以小分子化合物为靶点的药物，主要就是酪氨酸激酶以及酪氨酸激酶抑制剂，而本次论文主要就是研究这类酪氨酸激酶抑制剂、酪氨酸激酶，通过2-氟-4-硝基苯胺和8-溴辛酸乙酯为原料通过一系列回流和还原反应得到最终产物，并进行核磁检测研究其特性。31033
毕业论文关键词：靶向型抗肿瘤；酪氨酸激酶抑制剂；酪氨酸激酶；4-苯胺喹唑啉衍生物
The synthesis of A potential anti-tumor lead compound N - (3 - fluoro - 4 - (7) hydroxyl oxime acid) - heptyl amino benzene) - 6, 7 - dimethoxy quinazoline - 4 - amine synthesis
Abstract:The treatment of tumor has been a worldwide problem, it has been plagued by people's health, and it has been closely watched.With the development and popularization of  knowledge of medical and health and modern medical technology, the studies on new  potential anti-tumor drugs has received more and more attention.This kind of new type targeted anti-tumor drugs continuously change and it provides a new direction for future cancer therapy,Now the development of crystal diffraction technique, combination chemistry, molecular model technology promote the development of this kind of drugs.4 - aniline quinazoline derivatives is a kind of highly efficient hetero-cyclic compound,good biological activity is showed in the anti-bacterial, anti-tumor and anti-virus.One targeted anti-tumor drugs is made small molecular compounds as the target, it is mainly tyrosine kinase and tyrosine kinase inhibitors.And this paper is mainly to study this kind of tyrosine kinase inhibitors and tyrosine kinase,This experiment use 2 - fluoro - 4 - nitroaniline and 8 - bromine octylic acid ethyl ester as raw material to get the final product through reflux and reduction reaction.And then we use nuclear magnetic detection to study its properties.
Keywords: targeted anti tumor; tyrosine kinase inhibitors; tyrosine kinase; 4- aniline quinazoline derivatives
目录
1 前言    1
1.1 抗肿瘤药的研究进展与背景    1
1.2 靶向抗肿瘤药的相关介绍以及现今的研究进程    2
1.2.1 靶向抗肿瘤药的简介    2
1.2.2 靶向抗肿瘤药的研究现状    3
1.3 酪氨酸激酶及酪氨酸激酶抑制剂的简介    4
1.3.1 酪氨酸激酶的简介以及主要的信号传导通道    4
1.3.2 酪氨酸激酶的信号传导    6
1.4 一些新型的抗肿瘤药的介绍    8
2 文献综述    10
2.1 实验基本操作介绍及典型实验介绍    10
2.2 方案确认    11
3 实验与结果讨论    13
3.1 实验仪器    13
3.2 实验试剂    13
3.3 实验过程    13
3.3.1 常用的溶剂干燥处理    13
3.3.2 芳胺的制备即8-（2-氟-4-硝基苯基氨基）辛酸乙酯    14
3.3.3 8-（4-氨基-2-氟-苯氨基）辛酸乙酯的合成    14
3.3.4 N-（3-氟-4-（辛酸乙酯）胺）-6，7-二甲氧基-4-胺喹唑啉的制备    14 抗肿瘤先导化合物N-（3-氟-4-（7-异羟肟酸）-庚胺基苯）-6,7-二甲氧基喹唑啉-4:http://www.youerw.com/yixue/lunwen_27050.html