| (3S,4S)-4-([R)-1-羰基乙基]-3-([R)-1-(t-丁基二甲基硅烷氧基)乙基]氮杂环丁烷-2-酮的合成 |
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| 引用本文： | 任学军,郑玉林,张道凌,管海英.(3S,4S)-4-([R)-1-羰基乙基]-3-([R)-1-(t-丁基二甲基硅烷氧基)乙基]氮杂环丁烷-2-酮的合成[J].中兽医医药杂志,2012,31(2):20-21. |
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| 作者姓名： | 任学军 郑玉林 张道凌 管海英 |
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| 作者单位： | 上海新亚药业有限公司,上海,201203 |
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| 基金项目： | 上海市科委科研计划项目 |
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| 摘 要： | 以4-乙酰氧基氮杂环丁酮(2)为母核,与手性合成辅助剂溴丙酰基-螺环2H-1,3-苯并噁嗪-2,1’-环己基]-3(4H)-酮(3)进行取代反应,水解得培南类关键中间体(3S,4S)-4-(R)-1-羰基乙基]-3-(R)-1-(t-丁基二甲基硅烷氧基)乙基]-2-丙内酰胺(1),总收率约为81%~87.6%以4-乙酰氧基氮杂环丁酮(2)计]。
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| 关 键 词： | 培南类 中间体 合成 |
Synthesis of（3S,4S）-4-[（1R）-1-Carboxyethyl]-3-[（1R）-1-（t-Buth-yldimethylsilyloxy）ethyl]-2-azetidione |
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| REN Xue-jun,ZHENG Yu-lin,ZHANG Dao-ling,GUAN Hai-ying.Synthesis of（3S,4S）-4-[（1R）-1-Carboxyethyl]-3-[（1R）-1-（t-Buth-yldimethylsilyloxy）ethyl]-2-azetidione[J].Journal of Traditional Chinese Veterinary Medicine,2012,31(2):20-21. |
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| Authors: | REN Xue-jun ZHENG Yu-lin ZHANG Dao-ling GUAN Hai-ying |
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| Institution: | (Shanghai New Asia Pharmaceutical Co.,Ltd,Shanghai 201203,China) |
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| Abstract: | The key penems intermediate of（3S,4S）-4-（1R）-1-Carboxyethyl]-3-（1R）-1-（t-Buthyldime-thylsilyloxy） ethyl]-2-azetidione was synthesized from（3S,4R）-4-Acetoxy-3-（R）-1-（tert-butyldimethylsilyl-oxy）ethyl]azetidin-2-one with chiral synthesis auxiliary agent 3-（2-bromopropanoyl）spirobenzoe]o-xazine-2,1＇-cyclohexan]-4（3H）-one by substitution reaction,followed by hydrolysis.The overall yield was about 81%~87.6%（based on compound 2）. |
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| Keywords: | bovine clinical mastitis pathogenic bacteria isolation identification drug sensitive test |
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