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发明公开
CN1827610A 一种4位－酰基取代－2－甲基哌嗪化合物的制备方法 有权 转让 许可

一种4位－酰基取代－2－甲基哌嗪化合物的制备方法
摘要：
本发明涉及应用N，N’碳酰二咪唑(CDI)活化羧酸制备选择性单酰化哌嗪的方法，尤其是在2－甲基哌嗪环的4位氮原子上选择性单酰化反应制备一种4位－酰基取代－2－甲基哌嗪化合物的方法。其特征在于N，N’碳酰二咪唑与羧酸反应制成羰基二咪唑衍生物，再与2－甲基哌嗪进行单酰化缩合反应生成单酰化的4位－酰基取代－2－甲基哌嗪化合物。本发明的方法与现有技术相比，采用了价廉易得且易于工业化生产的N，N’碳酰二咪唑作为二乙基氯化铝的有效替代试剂，从源头上消除了安全隐患，避开了易燃易爆的二乙基氯化铝，操作方便，反应收率高。
摘要（英）：

The invention relates to a method for preparation of selective monoacylated piperazine by N,Ní»-carbonyldiimidazole(CDI) activating carboxyl acid and especially to a method for preparation of 4-acylsubstitution-2-methylpiperazine compound by selectively monoacylating 4-nitrogen atom of 2-methylpiperazine ring.It is characterized in that it prepares carbonyl diimidazolederivant by the reaction of between N,Ní»-carbonyldiimidazole and carboxyl acid, and monoacylated 4-acylsubstitution-2-methylpiperazine compound is obtained by monoacylated condensation reaction between 2-methylpiperazine and the substances of the former step. In relation to the present technology, the said invention selects N,Ní»-carbonyldiimidazole which is cheap and easy for commercial manufacture as effective substitute agent of diethyl aluminium chloride, essentially removes potential safety hazard, avoids the explosive diethyl aluminium chloride, and is of simple operation and high reaction yield rate.

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