| 2-氨基(芳氧基)-3-对甲基苯基噻吩并[3',2':5,6]吡啶并[4,3-d]嘧啶-4(3H)-酮的合成和生物活性 |
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| 引用本文： | 刘建超,贺红武,陈荷莲. 2-氨基(芳氧基)-3-对甲基苯基噻吩并[3',2':5,6]吡啶并[4,3-d]嘧啶-4(3H)-酮的合成和生物活性[J]. 有机化学, 2011, 31(8) |
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| 作者姓名： | 刘建超 贺红武 陈荷莲 |
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| 作者单位： | 华中师范大学化学学院农药与化学生物学教育部重点实验室 武汉430079 |
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| 基金项目： | 国家自然科学基金(Nos.20372023,20772042); 国家重点基础研究发展(973计划)规划(No.2010CB126100); 教育部创新团队部分(No.IRT0953)资助项目 |
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| 摘 要： | 用邻氨基噻吩腈与乙酰乙酸甲酯为原料,利用串联Aza-Wittig法合成了9个未见文献报道的噻吩并吡啶并嘧啶类化合物,通过IR,1H NMR,EI-MS,元素分析等方法对所合成的化合物进行了结构表征,并初步测定了所合成化合物的杀菌活性.生测结果表明:此类化合物对棉花枯萎(Fusarium oxysporium)、水稻纹枯(Rhizoctonia solani)、小麦赤霉(Gibberella zeae)、苹果轮纹菌(Dothiorella gregaria)、棉花炭疽菌(Colletotrichum gossypii)等5种菌均有一定的抑制活性.其中对苹果轮纹菌抑制活性最好,在浓度为5.0×10-5g/mL时抑制率为31.80%～82.84%.
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| 关 键 词： | 乙酰乙酸甲酯 Aza-Wittig法 噻吩并吡啶 吡啶并嘧啶 杀菌活性 |
Synthesis and Fungicidal Activities of 2-(Amino/acetoxy)-3-(4-methylphenyl)-thieno[3',2':5,6]pyrido[4,3-d]-pyrimidin-4(3H)-one Derivatives |
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| Liu Jianchao,He Hongwu,Chen Helian. Synthesis and Fungicidal Activities of 2-(Amino/acetoxy)-3-(4-methylphenyl)-thieno[3',2':5,6]pyrido[4,3-d]-pyrimidin-4(3H)-one Derivatives[J]. Chinese Journal of Organic Chemistry, 2011, 31(8) |
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| Authors: | Liu Jianchao He Hongwu Chen Helian |
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| Affiliation: | Liu,Jianchao He,Hongwu* Chen,Helian(Key Laboratory of Pesticide and Chemical Biology of Ministry of Education,College of Chemistry,Central China Normal University,Wuhan 430079) |
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| Abstract: | A novel facile synthetic method for thienopyridine derivatives was proposed via the reaction of 2-amino-thiophenes with acetoacetic ester and tin tetrachloride under heating.A series of new 2-(amino/acetoxy)-3-(4-methylphenyl)-thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-one derivatives had been designed and synthesized via an aza-Wittig reaction and structually confirmed by IR,1H NMR,EI-MS techniques,and elemental analysis.Their biological activities were also researched and many of them showed fungicidal... |
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| Keywords: | acetoacetic ester aza-Wittig reaction thienopyridine pyrido[4 3-d]pyrimidine fungicidal activity |
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