| 医药中间体(3R,4R)-3-[(1R)叔丁基二甲基硅氧乙基]-4-乙酰氧基-2-氮杂环丁酮的合成 |
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| 引用本文： | 章文军,赵昕.医药中间体(3R,4R)-3-[(1R)叔丁基二甲基硅氧乙基]-4-乙酰氧基-2-氮杂环丁酮的合成[J].应用化工,2008,37(4):361-363. |
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| 作者姓名： | 章文军 赵昕 |
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| 作者单位： | 河北工业大学,化工学院,天津,300130 |
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| 摘 要： | 以6-氨基青霉烷酸(6-APA)为原料经重氮化、溴化、酯化、还原、开环、氧化反应得到目标产物医药中间体(3R,4R)-3-(1R)叔丁基二甲基硅氧乙基]-4-乙酰氧基-2-氮杂环丁酮。经1H NMR,IR证明得到了氮杂环丁酮,提高了酯化反应的收率,改变了格氏试剂反应中苛刻的条件,降低了开环反应的温度并提高了开环收率,总收率为35.88%。
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| 关 键 词： | 氮杂环丁酮 抗生素 青霉烯 合成 |
| 文章编号： | 1671-3206(2008)04-0361-02 |
| 修稿时间： | 2008年2月28日 |
Synthesis of (3R,4R)-4-acetoxy-3-[(R)-1-(t-butyldimethylsilyloxy)ethyl]-2-azetidinone |
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| ZHANG Wen-jun,ZHAO Xin.Synthesis of (3R,4R)-4-acetoxy-3-[(R)-1-(t-butyldimethylsilyloxy)ethyl]-2-azetidinone[J].Applied chemical industry,2008,37(4):361-363. |
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| Authors: | ZHANG Wen-jun ZHAO Xin |
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| Abstract: | (3R,4R)-4-Acetoxy-3-(R)-1-(t-butyldimethylsilyloxy)ethyl]-2-azetidinone was synthesized by diazotized and brominated of 6-APA followed by esterification,deoxidize,cleavage and oxidation with an overall yield of about 35.88% and was proved by 1H NMR and IR.Increased the production rate of esterification.Changed the condition of Grignard reagent reaction.Reduced the temperature of cleavage and increased the production rate. |
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| Keywords: | azetidinone antibiotics penem synthesis |
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