新型5-取代吲哚-3-甲酰胺化合物的合成 |
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引用本文: | 焦林如,王新颖,刘益州,康从民.新型5-取代吲哚-3-甲酰胺化合物的合成[J].合成化学,2016,24(8):697-700. |
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作者姓名: | 焦林如 王新颖 刘益州 康从民 |
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作者单位: | 青岛科技大学 化工学院,山东 青岛 266042 |
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基金项目: | 国家自然科学基金资助项目(21072111,21272131) |
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摘 要: | 以5-取代吲哚为原料,经维尔斯迈尔-哈克反应制得5-取代吲哚-3-甲醛(2a~2e); 2a~2e在DMF催化下,与盐酸羟胺反应制得5-取代吲哚-3-甲腈(3a~3e); 3a~3e在H2O2和NaOH溶液中水解合成了5-取代吲哚-3-甲酰胺(4a~4e, 4b~4e为新化合物),产率62.0%~75.0%,其结构经1H NMR, 13C NMR和ESI-MS表征。
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关 键 词: | 5-取代吲哚 5-取代吲哚-3-甲酰胺 中间体合成 |
收稿时间: | 2016-01-19 |
Synthesis of Novel 5-Substituted-1 H-indole-3-carboxamides |
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Abstract: | 5-Substitued-indole-3-formaldehydes(2a~2e) were prepared by Vilsmeier-Haack reaction from 5-substituted indoles.5-Substituted indole-3-methyl cyanides(3a~3e) were obtained by the re-action of 2a~2e with hydroxylamine hydrochloride, using DMF as catalyst.5-Substituted indole-3-car-boxamides(4a~4e, 4b~4e were novel compounds) with yield of 62.0%~75.0% were synthesized by hydrolyzation of 3a~3e in H2 O2-NaOH solution.The structures were characterized by 1 H NMR, 13 C NMR and ESI-MS. |
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Keywords: | 5-substitued indole 5-substituted indole-3-carboxamide intermediate synthesis |
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