比拉斯汀重要中间体的合成

发布时间：2018-04-26 11:14

  本文选题：比拉斯汀 + 中间体　； 参考：《中国医药工业杂志》2016年11期

【摘要】：1-Boc-4-哌啶甲醇发生氧化反应得1-Boc-哌啶-4-甲醛,与2-硝基苯胺发生还原-闭环反应得4-(1H-苯并[d]咪唑-2-基)哌啶-1-羧酸叔丁酯,与2-氯乙基乙醚发生烷基化反应,再经水解得合成比拉斯汀的重要中间体1-(2-乙氧基-乙基)-2-哌啶-4-基-1H-苯并咪唑,总收率约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.
【作者单位】： 兰陵县人民医院;
【分类号】：R914.5
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本文编号：1805780