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[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。
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[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.
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