| 无溶剂Ugi四组分反应合成新型含氟Philanthotoxin-12衍生物及杀虫活性 |
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| 引用本文： | 刘年金,曹松,马严明,申丽,钱旭红.无溶剂Ugi四组分反应合成新型含氟Philanthotoxin-12衍生物及杀虫活性[J].应用化学,2009,26(10):1159-1164. |
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| 作者姓名： | 刘年金 曹松 马严明 申丽 钱旭红 |
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| 作者单位： | (上海市化学生物学重点实验室,华东理工大学药学院 氟化学工程中心 上海 200237) |
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| 基金项目： | 国家重点基础研究发展规划"九七三"项目 |
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| 摘 要： | 以无溶剂Ugi四组分反应合成关键含氟中间体，然后经三氟乙酸脱除保护基，合成了8个未见文献报道的新型含氟Philanthotoxin-12衍生物。重要的中间体和目标化合物的结构经1H NMR、13C NMR和HRMS或MS的确认。对目标化合物进行了初步的杀虫活性测试，其中含氟的化合物6b在100 mg/L浓度下对棉铃虫和菜青虫的杀死率分别为44%和42%。
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| 关 键 词： | Philanthotoxin 无溶剂合成 Ugi四组分反应 杀虫活性 |
| 收稿时间： | 2008-09-12 |
| 修稿时间： | 2008-12-18 |
Solvent-free Ugi Four-component Synthesis and Insecticidal Activities of Novel Fluorine-Containing Philanthotoxins-12 Derivatives |
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| LIU Nian-Jin,CAO Song,MA Yan-Ming,SHEN Li,QIAN Xu-Hong.Solvent-free Ugi Four-component Synthesis and Insecticidal Activities of Novel Fluorine-Containing Philanthotoxins-12 Derivatives[J].Chinese Journal of Applied Chemistry,2009,26(10):1159-1164. |
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| Authors: | LIU Nian-Jin CAO Song MA Yan-Ming SHEN Li QIAN Xu-Hong |
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| Affiliation: | (Shanghai Key Laboratory of Chemical Biology,Center of Fluorine Chemical Technology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237) |
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| Abstract: | Eight novel fluorine-containing PhTX-12 derivatives were prepared under one-pot Ugi four-component solvent-free conditions, followed by the simple removal of the protecting groups in the presence of trifluoroacetic acid. Their structures were identified by 1H NMR, 13C NMR and HRMS. Preliminary bioassays indicated that compound 6b showed 44% and 42% mortality rate against Heliothis armigera and Pieris rapae at a concentration of 100 mg/L. |
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| Keywords: | Philanthotoxin |
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