抗病毒药物更昔洛韦的合成与分析-药物化学专业毕业论文.docxVIP

囊汪太学疆圭学位论文摘要 囊汪太学疆圭学位论文 摘要 f ，一f更酱洛韦是新一代抗病毒药物，具有广谱 。t3 毒的作用。本文在综述文献合成方法的基础用 善先，磅交了良1,3-2．二氯-2．瓣辩先罪辩，缎絮c孚基纯、簸辱|二、缝合、零解 反应合成鞭昔洛韦的路线，重点考察了缩合反应巾各因素对缩含反应异构体嫩成 比例的影响，发现仅通过改变反应祭件很难实现异构体的完全转化。 在舅一方法孛，零论文采薅苯攀蔑基蓥馋裂链彀钱薹，遴j窭经隧效疲壤麓 14-9异构体的生成比例。首先以1，3一二氯一2一丙醇为原料，缀甲氧基甲籀化、 酯化、乙酰化反应合成l，3．二苯甲酰氧基-2．丙载基甲醇醋酸黼，并优化了备部 反应条昝，总浚率鸯64．3％。憝爱嚣毒双z}魏骞潆岭迸霞绩合爱应，隶瓣魏爨护 得到了鼹背洛韦纯品。讨论了催化剂种类及用量、反应时间、腮应温度、物料配 比等因索对缩合反应异构体生成的影响。该路线以l，3一二絮c一2一丙醇计爨收 率32％，戳DAG诗篱牧率主}争50％。该路线墨艺蔗萃、舔辩易褥、牧攀离、 成本低，适合工业化生产。 关键词：更营洛韦；．合成；位阻效威；l，3-----苯甲酰氧基-2-冈氧基甲醇醋酸醑； 双己酰鸟嘌呤 浙茳大学硬±掌穰论文A辩s，rRACT 浙茳大学硬±掌穰论文 A辩s，rRACT Gancictovir is a rLovel class of nueleoside analogues which is a potent and broad-acting(herpes simplex virus types i and 2，cytomegalovims,and Epstein-Barr virus)antiherpetic agent。 Based on the review of the literatures，Two synthesis routes of ganciclovir are described． The first route：the ganciclovir is synthesized t妇ough chloromethylation,es terifieaton,condensation and hydrolyzation from 1,3qiickloro-2-pmpanol，And th e condensation reacting condition is optimized,but the result is not ideal． Tho second route is a novel and industrially advantageous process for synt hesizing ganciclovir,which obtains the pure ganciclovir by adding the space St eric effect tO the by-side chain．曩撵synthetic routo comprises five re．action ste ps：methoxymethylation，esterification,acetOxylation,condensation，transp矗．nati on and hydrolyzation．The total yield is 32％． In addition，we have tried a llew synthetic method of 3AC through metho xymethylation．estylation,acetylation。n圮total yield amounts tO 64％．We also research the synthesis of diaeetylganunine with gnanine,with 92％yield． 鞭e synthesis process of gancilovir Was simpler than that of documents reported，and the react condition is moderate。the chemical structum ofthe product was confirmed by IR)H-NMR and MS Key Words：ganciclovir；synthesis；space steric effect；N2,Ng．diacetylganciguine； 2-(Acetoxymethoxy)-l,3-pr-opanediyl Dibenzoate 噩 鞭莲天学疆士掌霞论文第1辈文麸综述 鞭莲天学疆士掌霞论文 第1辈文麸综述 {。{撬病毒药物的冒内羚发展动态 抗病毒炎药物