| Lipozyme TL IM催化合成Temsirolimus |
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| 引用本文： | 万振江,卢晓霞.Lipozyme TL IM催化合成Temsirolimus[J].合成化学,2012,20(2):248-250,259. |
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| 作者姓名： | 万振江 卢晓霞 |
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| 作者单位： | 中国科学院成都生物研究所天然产物研究中心,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： | 在脂肪酶Lipozyme TL IM的催化下,2,2,5-三甲基-1,3-二氧六环-5-羧酸酐对抗生素西罗莫司的42-位羟基进行区域选择性酯化制得化合物4;4水解后合成了西罗莫司脂化物Temsirolimus,总产率83.7%。其结构经1H NMR和HR-MS确证。
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| 关 键 词： | 西罗莫司 Lipozyme TL IM Temsirolimus 酯化反应 药物合成 |
Catalytic Synthesis of Temsirolimus by Lipozyme TL IM |
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| WAN Zhen-jiang
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LU Xiao-xia.Catalytic Synthesis of Temsirolimus by Lipozyme TL IM[J].Chinese Journal of Synthetic Chemistry,2012,20(2):248-250,259. |
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| Authors: | WAN Zhen-jiang LU Xiao-xia |
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| Institution: | (Natural Products Research Center,Chengdu Institute of Biology, Chinese Academy of Sciences,Chengdu 610041,China) |
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| Abstract: | Temsirolimus was prepared by regioselective esterification at the 42-hydroxy of sirolimus using 2,2,5-trimethyl-1,3-dioxane-5-carboxylic anhydride as the esterifying agent and Lipozyme TL IM as the catalyst to give intermediate 4,followed by hydrolysis.The total yield was 83.7% and the structure was confirmed by 1H NMR and HR-MS. |
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| Keywords: | sirolimus Lipozyme TL IM temsirolimus esterification drug synthesis |
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