| 药物中间体(R)-3-氨基哌啶二(三氟乙酸)盐的合成 |
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| 引用本文： | 刘婷婷,邓瑞红,杜艳霞,刘文中,林森.药物中间体(R)-3-氨基哌啶二(三氟乙酸)盐的合成[J].南昌大学学报(工科版),2014(2):129-132. |
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| 作者姓名： | 刘婷婷 邓瑞红 杜艳霞 刘文中 林森 |
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| 作者单位： | [1]南昌大学化学系,江西南昌330031 [2]上海阳帆医药科技有限公司,上海201203 |
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| 摘 要： | 以(R)-2-((苄氧羰基)氨基)-1,5-戊二醇(1)为原料,通过酯化、环合、催化氢化、成盐反应,合成了药物中间体(R)-3-氨基哌啶二(三氟乙酸)盐(5);其结构经1H NMR、13C NMR、IR和元素分析表征。该方法具有成本较低、反应条件温和、易操作等特点,有利于工业化生产。
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| 关 键 词： | (R)-2-((苄氧羰基)氨基)-1 5-戊二醇 (R)-3-氨基哌啶二(三氟乙酸)盐 合成 盐酸羟胺 |
Synthesis of（R）-3-aminopiperidine ditrifluoroacetate |
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| LIU Ting-ting,DENG Rui-hong,DU Yan-xia,LIU Wen-zhong,LIN Sen.Synthesis of（R）-3-aminopiperidine ditrifluoroacetate[J].Journal of Nanchang University(Engineering & Technology Edition),2014(2):129-132. |
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| Authors: | LIU Ting-ting DENG Rui-hong DU Yan-xia LIU Wen-zhong LIN Sen |
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| Affiliation: | 1. Department of Chemistry, Nanchang University, Nanchang 330031, China; 2. Shanghai Yangfan Pharmaceutical Technology Co. , Ltd, Shanghai 201203, China) |
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| Abstract: | Drug intermediates of（R）-3-aminopiperdine ditrifluoroacetate was synthesized by using（R）-2-carbobenzoxyamino-1,5-pentanediol as raw materials, through esterification, cyclization, catalytic hydrogenation and salification reaction. And the structure of（R）-3-aminopiperdine ditrifluoroacetate was characterized by 1H NMR, 13C NMR, IR and elemental analysis. The results showed that this method has low cost, mild reaction condition, easy operation and is suitable for production in industrial scale. |
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| Keywords: | （ R ） -2-carbobenzoxyamino-1 5-pentanediol （ R ） -3-aminopiperidine ditrifluoroacetate synthesis hydroxylamine hydrochloride |
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