姜凡伟,康从民.化学通报,2015,78(4):378-380. |
取代吲哚-3-甲酸类化合物的合成 |
Synthesis of Substituted Indole-3-carboxylic acid Derivatives |
投稿时间:2014-07-22 修订日期:2014-09-10 |
DOI: |
中文关键词: 取代邻硝基甲苯 取代吲哚-3-甲酸 三氟乙酸酐 |
英文关键词:Substituted 2-nitrotoluene, Substituted Indole-3-carboxylic acid, Trifluoroacetic Anhydride |
基金项目:国家自然科学基金项目(21072111、21272131)资助 |
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中文摘要: |
吲哚-3-甲酸是一种重要的有机中间体,被广泛的应用于医药与农药的合成。以取代邻硝基甲苯为原料,与N,N-二甲基甲酰胺二甲缩醛(DMFDMA)反应制得取代的2-硝基-β-二甲氨基苯乙烯,再经铁粉和乙酸还原环合制得取代吲哚,取代吲哚与三氟乙酸酐反应然后碱性条件下水解制得5种新型的取代吲哚-3-甲酸类化合物,该合成方法操作简单、条件温和、收率较高。 |
英文摘要: |
Indole-3-carboxylic acid was an important organic intermediate, which was widely used in the synthesis of medicine and pesticide. Substituted 2-nitro-β-dimethylamino styrene, obtained from the reaction of substituted 2-nitrotoluene, N,N-dimethylformamide dimethyl acetal in solvent of N,N-dimethylformamide, reacted with iron and acetic acid producing substituted indoles. The five novel substituted indole-3-carboxylic acids were synthesized from substituted indoles and trifluoroacetic anhydride. The reported synthesis had the advantages of simple post treatment, mild conditions and higher yields. |
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