目的 對6-甲氧基-7-[(1-甲基-4-哌啶)甲氧基]-4(3H)-喹唑啉酮的合成工藝進(jìn)行研究。方法 以1-叔丁氧羰基-4-對甲苯磺酰氧甲基哌啶和香草酸甲酯為起始原料，經(jīng)過脫叔丁氧羰基、甲基化、硝化、還原，最后經(jīng)Niementowski環(huán)合得到。結(jié)果 實(shí)驗(yàn)總收率約為56%。結(jié)論 優(yōu)化的新工藝減少了反應(yīng)步驟、降低了制備成本、簡化了反應(yīng)操作條件、提高了產(chǎn)率，更適合工業(yè)化生產(chǎn)。

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.