| O,O'-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性 |
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| 引用本文： | 王伟,张国平,宋宝安,汪华金林红,胡德禹,杨松. O,O'-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性[J]. 有机化学, 2007, 26(2): 279-284 |
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| 作者姓名： | 王伟 张国平 宋宝安 汪华金林红 胡德禹 杨松 |
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| 作者单位： | 贵州大学精细化工研究开发中心教育部绿色农药和农业生物工程重点实验室,贵阳550025 |
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| 基金项目： | 国家自然科学基金（No.20362004）、高等学校博士学科点专项科研基金（No.20040657003）和教育部新世纪优秀人才计划（No.NCET-04-0912）资助项目. |
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| 摘 要： | 采用无溶剂无催化剂合成方法, 分别进行了以O,O'-二烷基亚磷酸酯、3,4,5-三甲氧基苯甲醛、2-氨基取代苯并噻唑为原料的类Mannich一锅法合成反应研究, 经合成筛选, 优选出控制反应温度100 ℃, 无溶剂、无催化剂加热反应120 min的合成方法, 实验结果表明该方法经济、简便、对环境友好. 经元素分析, IR, 1H NMR, 13C NMR对所合成的化合物进行了结构确认和表征. 培养并测定了化合物4a的晶体结构. 初步生物活性测试表明, 化合物具有一定的抗烟草花叶病毒活性.
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| 关 键 词： | α-氨基膦酸酯 苯并噻唑 合成 无溶剂无催化剂 抗烟草花叶病毒活性 |
| 收稿时间： | 2006-02-20 |
| 修稿时间： | 2006-02-20 |
Synthesis and Anti-Tobacco Mosaic Virus Activity of O,O'-Dialkyl- α-(substituted benzothia-zol-2-yl)amino-(substituted phenylmethyl)phosphonate |
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| WANG Wei, ZHANG Guo-Ping, SONG Bao-An, WANG Hua, JIN Lin-Hong, HU De-Yu, YANG Song. Synthesis and Anti-Tobacco Mosaic Virus Activity of O,O'-Dialkyl- α-(substituted benzothia-zol-2-yl)amino-(substituted phenylmethyl)phosphonate[J]. Chinese Journal of Organic Chemistry, 2007, 26(2): 279-284 |
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| Authors: | WANG Wei ZHANG Guo-Ping SONG Bao-An WANG Hua JIN Lin-Hong HU De-Yu YANG Song |
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| Affiliation: | Key Laboratory of Green Pesticide and Agricultural Bioengineering of Ministry of Education, Research and Development Center of Fine Chemicals, Guizhou University, Guiyang 550025 |
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| Abstract: | The Mannich-type addition of O,O'-dialkyphosphite to 3,4,5-trimethoxybenzaldehyde and 2-aminobenzothiazole was carried out in one pot by means of adopting solvent-catalyst free condition. The optimized condition is at 100 ℃ and 120 min without catalyst and solvent, which is economic, convenient, high yields and environment-friendly. Their structures were clearly established by elemental analysis, IR, 1H NMR and 13C NMR spectra. Single crystals of 4a have been obtained and determined. The bioassay of some compounds showed that they have moderate anti-tobacco mosaic virus (TMV) activity. |
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| Keywords: | a-aminophosphonate benzothiazole moiety synthesis solvent-catalyst free anti-TMV activity |
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