【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。更多还原

【Abstract】 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.更多还原