黄 迢,苏 佳,樊伊雯,王清河,吴明书.1-苄基-3-(2-H-吡唑-3-酮基)-3'-(2-H-1,2-二乙
氧甲酰肼基)-二取代氧化吲哚的合成[J].海南师范大学学报自科版,2019,32(4):368-372 |
1-苄基-3-(2-H-吡唑-3-酮基)-3'-(2-H-1,2-二乙
氧甲酰肼基)-二取代氧化吲哚的合成 |
Synthesis of Diethyl 1-(1-benzyl-2-oxo-3-(3-oxo-2,3-dihydro-1Hpyrazol-1-yl) indolin-3-yl) hydrazine-1,2-dicarboxylate |
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DOI:10.12051/j.issn.1674-4942.2019.04.003 |
中文关键词: 氧化吲哚 C-H活化 氨化反应 合成 |
英文关键词: oxindole C-H activation amination reaction synthesis |
基金项目:海南省研究生创新科研课题(Hys2018-220);大学生创新训练计划项目(306030201) |
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中文摘要: |
以3-(3-羟基吡唑基)氧化吲哚作为氨化反应的前体,偶氮二甲酸二乙酯作为氨化试
剂,在四氢呋喃溶剂中,一步合成3,3'-二取代的氧化吲哚衍生物。该方法通过C-H活化构建了CN键,同时优化了反应条件,探讨了温度、催化剂,溶剂对反应产率的影响。该合成反应具有操作简
便、高收率(95%)和产物易纯化等特点。 |
英文摘要: |
A 3,3'-disubstituted oxindole derivative was synthesized in tetrahydrofuran solvent by using α-(3-pyrazolinyl)
oxindole as precursor of ammoniation and diethyl azodicarbonate as ammoniation reagent. The method constructed C-N
bond by autoxidation C-H activation, which has the characteristics of simple operation, high yield and easy purification of
products. The reaction conditions were optimized, and the effects of temperature, catalyst and solvent on the reaction yield
were discussed. |
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