| 替比培南匹伏酯侧链的合成 |
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| 引用本文： | 黄小光,黄冰娥,朱少璇.替比培南匹伏酯侧链的合成[J].中国新药杂志,2012(4):428-430. |
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| 作者姓名： | 黄小光 黄冰娥 朱少璇 |
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| 作者单位： | 广州白云山制药股份有限公司广州白云山制药总厂 |
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| 摘 要： | 目的:合成替比培南匹伏酯侧链1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐。方法:以2-甲硫基-2-噻唑啉为原料,经与3-羟基吖丁啶盐酸盐,甲烷磺酰氯,硫代乙酸钾以及水解4步反应合成1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐。结果:合成了1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐,总收率42%。结论:本方法可以方便地得到替比培南匹伏酯侧链1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐,提高了反应收率,简化了操作,降低了成本。
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| 关 键 词： | 替比培南匹伏酯 1-(4 5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐 合成 |
Synthesis of the side chain of tebipenem pivoxil |
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| HUANG Xiao-guang,HUANG Bing-e,ZHU Shao-xuan.Synthesis of the side chain of tebipenem pivoxil[J].Chinese Journal of New Drugs,2012(4):428-430. |
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| Authors: | HUANG Xiao-guang HUANG Bing-e ZHU Shao-xuan |
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| Institution: | (Guangzhou Baiyunshan Pharmaceutical General Factory,Guangzhou Baiyunshan Pharmaceutical Co.,Ltd.,Guangzhou 510515,China) |
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| Abstract: | Objective: To synthesize the side chain 1-(4,5-dihydrothiazol-2-yl) azetidine-3-thiol hydrochloride of tebipenem pivoxil.Methods: 1-(4,5-Dihydrothiazol-2-yl) azetidine-3-thiol hydrochloride was prepared from 2-(methylthio)-4,5-dihydrothiazole by a 4-step process,i.e.successively reacted with 3-hydroxyazetidine hydrochloride,methanesulfonyl chloride,potassium ethanethioate and hydrolysis.Results: The total yield of 1-(4,5-dihydrothiazol-2-yl) azetidine-3-thiol hydrochloride was 42%.Conclusion: This method increases the yield of 1-(4,5-dihydrothiazol-2-yl) azetidine-3-thiol hydrochloride,simplifies the process and decreases the cost. |
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| Keywords: | tebipenem pivoxil 1-(4 5-dihydrothiazol-2-yl) azetidine-3-thiol hydrochloride synthesis |
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