摘要奥氮平又称再普乐(Olanzapine),是一种适用于精神分裂症或其他精神障碍急性期和日常服用药物,具有治疗和维持作用。4-氨基-2-甲基-10H-噻吩[2,3-b][1,5]-苯二氮杂䓬是目前工业上合成奥氮平的主要中间体,广大科学研究者对其合成的研究一直都十分得关注。但现今已有的合成方法中使用的氯化亚锡溶液毒性大,且反应过程用量多,三废的产生量较大,故本文采用一种新的合成方法以提高产率,并取得较好的社会效益和经济效益。48181
本文主要介绍了奥氮平的性质;以及一种在酸性条件下,用以2-(2-硝基苯胺基)-5-甲基噻吩-3-腈作为原料,用金属锡粉做还原剂,顺利得到产物4-氨基-2-甲基-10H-噻吩[2,3-b][1,5]-苯二氮杂䓬盐酸盐的方法,并且通过控制变量的方法确定了最佳条件,在此基础上对实验结果进行了分析。
Abstract
Olanzapine also known as Zyprexa (Olanzapine), is one for schizophrenia or other mental disorders in acute and daily medication, has a therapeutic effect and maintain.The 4-amino-2-methyl -10H- thiophene [2,3-b] [1,5] - benzodiazepine hydrochloride is the main intermediate on the industrial synthesis of olanzapine,the majority of scientific researchers have been focusing on the research on its synthesis.But today toxicity stannous solution synthesis methods have been used in large, and the amount of multi-reaction process, the larger the amount of waste generated, so this paper, a new synthetic method to improve yield and achieve better social and economic benefits.
This paper describes the nature of olanzapine;And one for 2- (2-nitroanilino) -5-methylthiophene-3-carbonitrile as starting material, under acidic conditions, the metal tin powder as the reducing agent, to give product 4-amino-2-methyl -10H- thiophene [2,3-b] [1,5] - benzodiazepine hydrochloride.And to determine the optimum conditions for the method of control variables, the experimental results are analyzed.
毕业论文关键词; 奥氮平; 金属锡; 有机合成;4-氨基-2-甲基-10H-噻吩[2,3-b][1,5]-苯二氮杂䓬
Keyword: Olanzapine; Tin; Organic Synthesis;4-amino-2-methyl-10H-thiophene[2,3-b][1,5]-benzodiazepine hydrochloride;
目录
前言 4
1.实验背景概述 5
1.1奥氮平 5
1.1.1奥氮平的结构、性质 5
1.1.3奥氮平适用症状与不良反应 7
1.1.4奥氮平的国内外研究概况及发展趋势 7
1.1.5奥氮平的未来发展 8
1.2金属锡 8
2 .4-氨基-2-甲基-10H-噻吩[2,3-b][1,5]-苯二氮杂䓬的合成方法简介 9
2.1常用方法 9
2.2王亚平课题组的方法 10
2.3邹清华课题组的方法 10
3.实验部分 11
3.1实验仪器与试剂 11
3.1.1实验仪器 11
3.1.2实验试剂 11
3.2实验步骤 11
3.3实验结果讨论分析 12
3.3.1实验反应条件的优化 12
3.3.2.实验数据 15
4. 总结 15
结论与展望 16
致谢