温和条件下去丙酮保护制备末端单炔烃及末端二炔的方法
发布时间：2018-10-13 10:50
【摘要】：末端炔烃是有机合成中重要的原料或中间体.通过钯催化的Sonogashira偶联反应,将2-甲基-3-丁炔-2-醇连接到其它基团上所得到的结构,可以看作是一类丙酮保护的末端炔烃.目前,对于这种丙酮保护的末端炔烃,其去保护得到端基炔主要是通过KOH存在下在甲苯中回流数小时的方法,但是反应温度高,条件苛刻,适用范围较窄.对这一脱保护过程进行研究,通过对多种溶剂和反应温度进行对比,发现以1,4-二氧六环作为溶剂,KOH作为碱,可以在相对较低的温度(60℃)下得到较高的产率,而且所需时间大大缩短(0.5~2 h),拓展了这种方法的应用范围.
[Abstract]:Terminal alkynes are important raw materials or intermediates in organic synthesis. By palladium catalyzed Sonogashira coupling reaction, the structure of 2-methyl-3-butyne-2-ol linked to other groups can be regarded as a class of acetone-protected terminal alkynes. At present, for the terminal alkynes protected by acetone, the method of refluxing the terminal alkynes in toluene in the presence of KOH is the main method, but the reaction temperature is high, the conditions are harsh, and the range of application is narrow. Through the comparison of various solvents and reaction temperatures, it was found that the higher yield could be obtained at a relatively low temperature (60 鈩，
本文编号：2268343
[Abstract]:Terminal alkynes are important raw materials or intermediates in organic synthesis. By palladium catalyzed Sonogashira coupling reaction, the structure of 2-methyl-3-butyne-2-ol linked to other groups can be regarded as a class of acetone-protected terminal alkynes. At present, for the terminal alkynes protected by acetone, the method of refluxing the terminal alkynes in toluene in the presence of KOH is the main method, but the reaction temperature is high, the conditions are harsh, and the range of application is narrow. Through the comparison of various solvents and reaction temperatures, it was found that the higher yield could be obtained at a relatively low temperature (60 鈩，
本文编号：2268343
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