含氧乙二胺化合物单氨基保护工艺的研究

Study on Monoprotection Technology of Oxy-ethylenediamines

研究了一种通过构建酰胺对含氧乙二胺类化合物进行单氨基保护的策略,并对该工艺条件进行了方法学研究。在0℃温度下,待保护的含氧乙二胺衍生物与保护物(Boc)_(2)O的摩尔比例为8∶1,向反应体系中缓慢加入(Boc)_(2)O。该工艺方法得到70%左右的单氨基保护收率,且反应条件简单温和,工艺设备成本廉价,可对反应原料回收再利用,实现了操作简易、经济实惠和绿色环保的目的。

A strategy for monoamino protection of oxy-ethylenediamine compounds by constructing amides was studied,and the process conditions were also studied.At the temperature of 0℃,the molar ratio of the oxy-ethylene-diamine derivative to the protection(Boc)_(2)O was 8∶1,and(Boc)_(2)O was slowly added into the reaction system.The reaction conditions were simple and mild,the cost of process equipment was low,and the raw materials could be recovered and reused,which realized the purpose of simple operation,economic benefit and environmental protection.