Abstract: 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.