抗肿瘤药物吉非替尼的合成

《抗肿瘤药物吉非替尼的合成》由会员上传分享，免费在线阅读，更多相关内容在学术论文-天天文库。

1、授予单位代码１００８９学号或申请号１＾３＾巧（￡钟ＡＳＨｅｂｅｉＭｅｄｉｃａｌＵｎｉｖｅｒｓｉｔｙ硕±学位论文在职科学学位抗帥瘤药物吉非替尼的合成学位申请人：李建军导师；杜玉民教授专业：药物化学二级学院：药学院２０１５年１０月巧北医科大学学位论文使用授权及知巧产权归属承谱本学位论文在导师（或指导小组）的指导下，由本人独立完成。本学位论文研究所获得的研究成果，其知识产权归河北医科大学所有。河北医科大学有权对本学位论文进行交流、公开和使用。凡发表一署

2、名为单位河北医科大学与学位论文主要内容相关的论文，第，试验材料、原始数据、申报的专利等知识产权均归河北医科大学所有。否则，承担相应法律责任。研究生签名：李建＾师签章：若挺军泉等心負方屯．导ＰＭ‘河北医科大学研究生学位论文独创性声明本论文是在导师指导下进巧的研究工作及取得的研究成果，除了文中特别加Ｗ标巧和致谢等内容外，文中不包含其他人己经发表或撰写的研究成果。，指导教师对此进行了审定本论文由本人独立撰写，文责自负。研究生签名：导师签章：＞￡Ｐ１丈年一月日目录中文摘要········

3、····································································1英文摘要·········································································2英文缩写··············································································4研究论文抗肿瘤药物吉非替尼的合成前言·····················

4、····························································5材料与方法······································································10结果···············································································15附图··············································

5、·································16附表···············································································18讨论···············································································23结论··································································

6、·············28参考文献·········································································29综述表皮生长因子受体酪氨酸激酶抑制剂的研究进展···················30致谢··················································································40个人简历·········································

7、····································41中文摘要抗肿瘤药物吉非替尼的合成摘要吉非替尼，化学名为N-(3-氯-4-氟苯基)-7-甲氧基-6-[3-(吗啉-4-基)丙氧基]-喹唑啉-4-胺，是由阿斯利康公司研制的表皮生长因子受体酪氨酸激酶抑制剂，主要用于治疗非小细胞肺癌。本论文旨在探索出一条适宜工业化生产的吉非替尼合成路线，降低生产成本，减轻患者的经济负担。目的：建立并优化吉非替尼的制备方法。方法：在参考相关文献基础上，设计吉非替尼的合成路线。以3,4-二甲氧基苯甲酸(Ⅱ)为起始原料，先经硝化得到2-

8、硝基-4,5-二甲氧基苯甲酸(Ⅲ)，在碱性条件下脱甲基得到2-硝基-4-甲氧基-5-羟基苯甲酸(Ⅳ)，之后在氯化亚砜催化下与乙醇发生酯化反应得到2-硝基-4-甲氧基-5-羟基苯甲酸甲酯(Ⅴ)，中间体(Ⅴ)与4-(3-氯丙基)吗啉在碱性