碱催化醛、丙二腈和邻苯二甲酰肼的、三组分反应合成酞嗪衍生物

Synthesis of Pyridazine Derivatives by Base-Catalyzed Three-Component Reaction of Aldehyde,Malononitrile and Phthalhydrazide

经过实验验证引入水有利于芳香醛、丙二腈和邻苯二甲酰肼三组分的反应进行,催化量的有机碱三乙胺(Et 3 N)或无机碱磷酸氢二钾(K 2 HPO 4[DK1]·3H 2 O)可以在常规条件下促进该反应。本文以39%~97%的产率合成一系列1 H-吡唑[1,2-b]酞嗪-5,10-二酮衍生物。两种催化剂均溶于水,因此,反应结束后催化剂的分离与产物提纯简便易行。此方法具有反应条件温和、绿色环保、操作简单、后处理方便等特点。

Catalytic amount of organic base triethylamine(Et 3 N)or inorganic base dipotassium hydrogen phosphate(K 2 HPO 4[DK1]·3H 2 O)is proved to effectively promote the three components reaction of aromatic aldehyde,malononitrile and phthalhydrazide under conventional heating conditions.As expected,introduction of water is favorable to the reaction.A series of 1 H-pyrazole[1,2-b]pyridazine-5,10-diones derivatives was synthesized in the yield of 39%~97%.Both catalysts are soluble in water,and introduction of water also facilitate the separation of the catalyst after reaction.This approach also has advantages of mild reaction conditions,green environmental protection,simple operation and convenient post-treatment.