本文選題：比拉斯汀 + 中間體　； 參考：《中國醫(yī)藥工業(yè)雜志》2016年11期

【摘要】：1-Boc-4-哌啶甲醇發(fā)生氧化反應(yīng)得1-Boc-哌啶-4-甲醛,與2-硝基苯胺發(fā)生還原-閉環(huán)反應(yīng)得4-(1H-苯并[d]咪唑-2-基)哌啶-1-羧酸叔丁酯,與2-氯乙基乙醚發(fā)生烷基化反應(yīng),再經(jīng)水解得合成比拉斯汀的重要中間體1-(2-乙氧基-乙基)-2-哌啶-4-基-1H-苯并咪唑,總收率約73%。
[Abstract]:1-Boc-4-piperidine-4formaldehyde was obtained by oxidation of 1-Boc-4piperidine methanol, and then by reduction-closed-loop reaction with 2-nitroaniline to obtain 4-oc-1H-benzo [d] imidazole-2-yl) piperido-1-carboxylate tert-butyl ester, which was alkylated with 2-chloroethyl ether, After hydrolysis, the important intermediate of Pilastine was synthesized with the total yield of 73%, which was about 73.The main intermediate was 1-N 2-ethoxy-ethoxy-2-piperidine-2-piperidine-1H-benzimidazole.
【作者單位】： 蘭陵縣人民醫(yī)院;
【分類號】：R914.5
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本文編號：1805780