| Migrastatin母核9-羟基的衍生化 |
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| 引用本文： | 钟川龙,辜玲慧,吴小艾,范成中.Migrastatin母核9-羟基的衍生化[J].合成化学,2012,20(3):328-330,355. |
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| 作者姓名： | 钟川龙 辜玲慧 吴小艾 范成中 |
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| 作者单位： | 1. 四川大学华西药学院靶向药物教育部重点实验室,四川成都,610041
2. 四川大学华西医院核医学科,四川成都,610041 |
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| 基金项目： | 国家自然科学基金资助项目 |
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| 摘 要： | 为了将示踪元素引入Migrastatin母核并用于肿瘤诊断和靶向治疗,以2,6-二烯庚酸-5-(叔丁基二甲硅氧基)-6-甲氧基-2,4-二甲基-2,7-二烯酯为起始原料,经过脱TBS保护、酯化和烯烃复分解反应,成功地合成了Migrastatin母核9-甲磺酸酯,总收率15.3%,其结构经1H NMR和ESI-MS表征。
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| 关 键 词： | Migrastatin 示踪元素 靶向试剂 羟基酯化 烯烃复分解 合成 |
9-Hydroxyl Derivation of Migrastatin Core |
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| ZHONG Chuan-long
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GU Ling-hui
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WU Xiao-ai
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FAN Cheng-zhong.9-Hydroxyl Derivation of Migrastatin Core[J].Chinese Journal of Synthetic Chemistry,2012,20(3):328-330,355. |
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| Authors: | ZHONG Chuan-long GU Ling-hui WU Xiao-ai FAN Cheng-zhong |
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| Institution: | 1b(a.Key Laboratory of Drug-Targeting of Education Ministry of China,West China School of Pharmacy; b.Department of Nuclear Medicine,West China Hospital,1.Sichuan University,Chengdu 610041,China) |
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| Abstract: | The trace elements are introduced into the Migrastatin core and used it as the targeted agents for cancer diagnosis and treatment.9-Methanesulfonate of Migrastatin core was synthesized from(E)-(Z)-5-(t-butyldimethylsilyloxy)-6-methoxy-2,4-dimethylocta-2,7-dienyl]hepta-2,6-dienoate by a three-step reaction of deprotection of TBS,esterification and olefin metathesis in total yield of 15.3%.The structure was characterized by 1H NMR and ESI-MS. |
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| Keywords: | Migrastatin trace element targeted agent esterification of hydroxyl olefin metathesis synthesis |
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