王清清, 梁颖, 祝晓光. 医药中间体吡啶-2-硼酸的制备方法研究[J]. 蚌埠医学院学报, 2010, 35(10): 1043-1045.
    引用本文: 王清清, 梁颖, 祝晓光. 医药中间体吡啶-2-硼酸的制备方法研究[J]. 蚌埠医学院学报, 2010, 35(10): 1043-1045.
    WANG Qing-qing, LIANG Ying, ZHU Xiao-guang. Preparation of 2-pyridylboronic acid[J]. Journal of Bengbu Medical College, 2010, 35(10): 1043-1045.
    Citation: WANG Qing-qing, LIANG Ying, ZHU Xiao-guang. Preparation of 2-pyridylboronic acid[J]. Journal of Bengbu Medical College, 2010, 35(10): 1043-1045.

    医药中间体吡啶-2-硼酸的制备方法研究

    Preparation of 2-pyridylboronic acid

    • 摘要: 目的:探讨医药中间体吡啶-2-硼酸的制备方法。方法:以异丙基氯化镁为格氏试剂,2-溴吡啶和硼酸三(三甲硅烷基)酯为原料,在氮气保护下,通过格氏反应合成目标产物,用核磁共振确认产物结构。结果:合成了吡啶-2-硼酸,确证了产物结构;优化反应条件为:物料比n(硼酸酯):n(2-溴吡啶)=2:1,反应温度0℃,反应时间3 h,水解温度0℃,总收率达67.7%。结论:采用格氏反应制备吡啶-2-硼酸,反应条件温和,产物收率较高,有助于吡啶类药物的开发和研究。

       

      Abstract: Objective:To investigate the means of preparing 2-pyridylboronic acid.Methods:The product was synthesized with 2-bromopyridine,tris-trimethylsilylborate and iPrMgCl as Grignard reagents under N2,and identified by 1H-NMR.Results:2-pyridylboronic acid was synthesized with the yield of 67.7% on conditions of n (tris-trimethylsilylborate):n (2-bromopyridine)=2:1;the reaction temperature was 0℃,the reaction time 3 hours and the hydrolysis temperature 0℃.Conclusions:2-pyridylboronic acid can be synthesized by Grignard reaction on moderate conditions with high yield,which may contribute to the study of pyridine drugs.

       

    /

    返回文章
    返回