| 吡啶甲基亚氨基噻(噁)唑烷的合成及生物活性 |
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| 引用本文： | 徐晓勇,陈刚,钱旭红. 吡啶甲基亚氨基噻(噁)唑烷的合成及生物活性[J]. 农药学学报, 2003, 5(1): 27-33 |
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| 作者姓名： | 徐晓勇 陈刚 钱旭红 |
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| 作者单位： | 1.华东理工大学 药物化工研究所,上海 200237 |
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| 基金项目： | 国家863资助项目(2001AA235011);上海市化学生物学(芳香杂环)重点实验室支持项目. |
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| 摘 要： | 根据天然海藻糖酶抑制剂的结构设计了一类吡啶甲基亚氨基噻(噁)唑烷化合物, 通过吡啶甲基异硫氰酸酯和相应的胺反应, 然后在盐酸或黄色氧化汞条件下关环,合成了吡啶甲基亚氨基噻唑烷和噁唑烷,其结构得到IR、1H NMR、HRMS的确证。测试了化合物对昆虫(家蝇)飞行的抑制能力。对影响合成反应的因素以及生测结果进行了讨论。
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| 关 键 词： | 噻唑烷 噁唑烷 合成 生物活性 异硫氰酸酯 |
| 文章编号： | 1008-7303(2003)01-0027-07 |
Synthesis and Bioactivities of Novel Substituted Pyridinylmethylimino-thiazolidines and Oxazolidines Derivatives |
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| XU Xiao-yong,CHEN Gang and QIAN Xu-hong. Synthesis and Bioactivities of Novel Substituted Pyridinylmethylimino-thiazolidines and Oxazolidines Derivatives[J]. Chinese Journal of Pesticide Science, 2003, 5(1): 27-33 |
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| Authors: | XU Xiao-yong CHEN Gang QIAN Xu-hong |
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| Affiliation: | 1.Institute of Pesticides and Pharmaceutical, East China University ofScience and Technology, Shanghai 200237, China2.State Key Laboratoryof Fine Chemicals, Dalian University of Technology, Dalian 116012,China |
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| Abstract: | Based on the structure of Trehazolin, one of natural trehalase inhibitors, pyridinylmethylimino thiazolidine and oxazolidine compounds were designed and synthesized through reaction of pyridinylmethyl isothiocyanate with appropriate amine and followed by cyclization under HCl and HgO. Their structures were confirmed by using IR, 1H NMR, HRMS. The insect flight inhibitory bioactivity was given. |
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| Keywords: | thiazolidines oxazolidine synthesis bioactivity isothiocyanate |
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