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3-胺基-丙基硼酸的合成

Synthesis of 3-Aminopropylboronic Acid
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摘要 硼酸类化合物可以选择性地抑制β-内酰胺酶的生成,从而提高β-内酰胺类抗生素的生物活性,因此成为目前研究的热点之一。以3-溴-丙基频哪醇硼酸酯为起始原料,经叠氮化反应、还原氢化反应以及脱保护三步反应合成了3-胺基-丙基硼酸,总收率为67.7%。同时采用1 H-NMR和MS对中间体以及目标化合物的结构进行了表征。 Abstract.Boronic acid has attracted great fl-lactamase to improve the biological interest due to the feature as the selective inhibitors of activity of the β-lactam antibiotics. In this paper, 3-aminopropylboronic acid was synthesized via azidation, hydrogenation reduction and deprotection reaction starting from 3-bromopropylboronic acid pinacol ester. The overall yield of the three-step reaction was 67.7 %. The intermediate products and target product were identified by 1H-NMR and MS.
出处 《上海应用技术学院学报(自然科学版)》 2012年第4期288-290,共3页 Journal of Shanghai Institute of Technology: Natural Science
基金 上海高校青年教师培养资助计划(yyy11026)
关键词 频哪醇硼酸酯 硼酸 叠氮化 氢化还原 boronic acid pinacol ester~ boronic acid azidation hydrogenation reduction
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