| 1-(1,3-噻唑啉-2-基)-3-巯基氮杂环丁烷盐酸盐的工艺研究 |
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| 引用本文： | 史颖,张雅然,底辉锋,贾铭,张志宝.1-(1,3-噻唑啉-2-基)-3-巯基氮杂环丁烷盐酸盐的工艺研究[J].化学试剂,2011,33(10):939-941. |
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| 作者姓名： | 史颖 张雅然 底辉锋 贾铭 张志宝 |
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| 作者单位： | 石药集团中奇制药技术(石家庄)有限公司,河北石家庄,050051 |
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| 基金项目： | “十一五”重大新药创制资助项目(2008ZX09401-004) |
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| 摘 要： | 以2-巯基-2-噻唑啉为起始原料,经过甲基化、与3-羟基氮杂环丁烷盐酸盐发生亲核取代SN2、甲磺酰氯活化羟基、与硫代乙酸钾发生亲核取代SN2、碱性水解5个反应步骤,合成目标产物,总收率51.6％,HPLC纯度98.5％.各中间体及终产品通过熔点、IR、1HNMR、MS等手段进行了结构确证.该方法反应条件温和、操作简便、...
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| 关 键 词： | 1-(1 3-噻唑啉-2-基)-3-巯基氮杂环丁烷盐酸盐 泰比培南酯 产业化 |
Synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine hydrochloride |
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| SHI Ying,ZHANG Ya-ran,DI Hui-feng,JIA Ming,ZHANG Zhi-bao.Synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine hydrochloride[J].Chemical Reagents,2011,33(10):939-941. |
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| Authors: | SHI Ying ZHANG Ya-ran DI Hui-feng JIA Ming ZHANG Zhi-bao |
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| Affiliation: | SHI Ying,ZHANG Ya-ran,DI Hui-feng,JIA Ming,ZHANG Zhi-bao (CSPC Zhongqi Pharmaceutical Technology(SJZ) Co.,LTD,Shijiazhuang 050051,China) |
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| Abstract: | 3-Mercapto-1-(1,3-thiazolin-2-yl)azetidine hydrochloride has been synthesized by taking 2-thiol-2-thiazoline as raw material,through methylation,nucleophilic substitution SN2 with 3-hydroxyazetidine hydrochloride,activation of hydroxyl with methanesulfonyl chloride,nucleophilic substitution SN2 with potassium thioacetate and basic hydrolysis.Total yield is 51.6%,and purity of product is 98.5%.The structures of intermediates and product have been characterized by melting point,IR,1HNMR and MS techniques.The ... |
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| Keywords: | 3-mercapto-1-(1 3-thiazolin-2-yl)azetidine hydrochloride tebipenem pivoxil industrialization |
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