6-甲氧基-7-[(1-甲基-4-哌啶)甲氧基]-4(3H)-喹唑啉酮的合成工艺研究  

Synthesis of 6-methoxy-7-[(1-methyl-4-piperidine)]-4(3H)-quinazolone

作　　者：李靖[1] 石玉[2] 李祎亮[2] 夏超[3] 魏会强[3] 宋晓凯[4] 

机构地区：[1]中国矿业大学,江苏徐州221116 [2]天津药物研究院天津市新药设计与药物发现重点实验室,天津300193 [3]天津大学,天津300192 [4]淮海工学院化学工程学院,江苏连云港222005

出　　处：《现代药物与临床》2013年第2期129-131,共3页Drugs & Clinic

摘　　要：目的对6-甲氧基-7-[(1-甲基-4-哌啶)甲氧基]-4(3H)-喹唑啉酮的合成工艺进行研究。方法以1-叔丁氧羰基-4-对甲苯磺酰氧甲基哌啶和香草酸甲酯为起始原料,经过脱叔丁氧羰基、甲基化、硝化、还原,最后经Niementowski环合得到。结果实验总收率约为56%。结论优化的新工艺减少了反应步骤、降低了制备成本、简化了反应操作条件、提高了产率,更适合工业化生产。Objective To study the synthetic technology of 6-methoxy-7-[（1-methyl-4-piperidine）methoxyl]-4（3H）-quinazolone.Metheds Taking tert-butyl 4-（（tosyloxy）methyl）piperidine-1-carboxylate and methyl vanillate as the starting material,target compound was obtained after a series of chemical reactions including stripped tert-butoxy carbonyl,methylation,nitrification,reducing reaction,and Niementowski cyclization.Results The overall yield was 56%.Conclusion The improved procedure could reduce the reaction steps and lower the cost of preparation,simplify the reaction operating conditions,increase the yield,and make it more suitable for the industrial requirements.

关 键 词：6-甲氧基-7-[(1-甲基-4-哌啶)甲氧基]-4(3H)-喹唑啉酮 硝化 Niementowski环合 

分 类 号：R914[医药卫生—药物化学]