多组分一锅法合成2-氨基吡咯衍生物

Multi-component one-pot synthesis of 2-aminopyrrole derivatives

建立了一种2-氨基吡咯衍生物的绿色合成方法,该方法以苯甲酰甲醛类化合物、1,1-烯二胺类化合物和2-羟基-1,4-萘醌为原料,在乙醇溶剂中,通过三组分一锅法串联反应合成8个多取代的2-氨基吡咯衍生物4a~4h,收率73%~78%.产物结构经1H NMR、13C NMR和HRMS表征.该方法具有环境友好、操作简单(过滤和洗涤,无柱色谱分离)、收率高、原料商品可得、目标化合物具有潜在生物活性等优点.

In this paper,the green synthesis method was constructed for synthesis of 2-aminopyrrole derivatives,which through multi-component one-pot cascade reaction of the arylglyoxal monohydrates 1,1,1-endiamines(EDAMs)2,and 2-hydroxynaphthalene-1,4-dione 3 in ethanol.As a result,a series of 2-aminopyrrole derivatives 4a−4h have been synthesized with 73%−78%yields by this one-step reaction.All products were newly synthesized and fully characterized by 1H NMR,13C NMR and HRMS.This approach has several advantages such as the use of an environmentally-friendly solvent,simple and practical operation(with filtration and washing and no column chromatography separation),good yields,use of commercially available raw materials,diverse target compounds,and products with potential biological activity.