精细化工中间体2024,Vol.54Issue(1) :46-48,69.DOI:10.19342/j.cnki.issn.1009-9212.2024.01.010

3-[(1-甲基-1H-吡咯-2-基)亚甲基]吲哚啉-2-酮的合成研究

Synthesis of 3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one

郑静静 广海东 陈莉莉 王永亮 门靖
精细化工中间体2024,Vol.54Issue(1) :46-48,69.DOI:10.19342/j.cnki.issn.1009-9212.2024.01.010

3-[(1-甲基-1H-吡咯-2-基)亚甲基]吲哚啉-2-酮的合成研究

Synthesis of 3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one

郑静静 1广海东 2陈莉莉 3王永亮 1门靖4
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作者信息

  • 1. 江苏承开中药有限公司,江苏淮安 211600
  • 2. 陕西省药品和疫苗检查中心汉中分中心,陕西汉中 723000
  • 3. 陕西大河药业有限责任公司,陕西西安 710200
  • 4. 西安万隆制药股份有限公司,陕西西安 710119
  • 折叠

摘要

以吲哚啉-2-酮和N-甲基-2-吡咯甲醛为起始原料,经Aldol缩合反应合成得到3-[(1-甲基-1H-吡咯-2-基)亚甲基]吲哚啉-2-酮.产物结构经核磁共振氢谱(1HNMR)和质谱(ESI-MS)确证,Aldol缩合反应的优化条件为:哌啶作为有机碱催化剂、物料比n(哌啶)∶n(N-甲基-2-吡咯甲醛)∶n(吲哚啉-2-酮)=0.2∶1.2∶1.0、反应溶剂为乙醇、反应温度80 ℃、反应时间5 h,优化条件下,产物收率达73.4%(以吲哚啉-2-酮计).

Abstract

3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one was synthesized from indoline-2-one and N-methyl-2-pyrrole-formaldehyde via Aldol condensation reaction.The structure of the product was characterized by proton NMR(1H NMR)and mass spectrometry(ESI-MS).The optimum conditions of the aldol condensation reaction were as follows:piperidine was used as the organic base catalyst;the molar ratio of materials was n(piperidine)∶n(N-methyl-2-pyrrole-formaldehyde)∶n(indoline-2-one)=0.2∶1.2∶1.0,the reaction solvent was ethanol,the reaction temperature was 80 ℃,and the reaction time was 5 h.A yield of product was up to 73.4%under these reaction conditions.

关键词

吲哚衍生物/舒尼替尼/Aldol缩合反应

Key words

indole derivatives/sunitinib/Aldol condensation reaction

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出版年

2024
精细化工中间体
湖南化工研究院

精细化工中间体

CSTPCD
影响因子:0.236
ISSN:1009-9212
参考文献量15
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