芳香胺、异硫氰酸酯和丁炔二酸二甲酯三组分反应合成噻唑-4-酮衍生物研究

Synthesis of Thiazolidin-4-one Derivatives by Three-component Reaction of Arylamines,Isothiocyanates and Dimethyl Acetylenedicarboxylate

噻唑-4-酮类化合物具有较好的生物活性,是非常好的有机合成中间体,可用于具有生物活性的化合物的合成。在无催化剂存在下,芳香胺、异硫氰酸酯和丁炔二酸二甲酯在乙醇中加热回流,高产率地生成了多取代噻唑-4-酮衍生物。共合成和鉴定了14个多取代噻唑-4-酮衍生物,并提供了该多组分反应的一个合理的多步连续反应机理。

Thiazole moiety-4-ketone compounds have good biological activity and very good organic synthesis intermediate,which can be used for the synthesis of bioactive compounds. In the absence of any catalyst,the three-component reaction of arylamines,isothiocyanates and dimethyl acetylenedicarboxylate in heating and refluxing ethanol is obtained,producing the polysubstituted thiazolidin-4-one derivatives in high yields. In this article,fourteen polysubstituted thiazolidin-4-one derivatives are efficiently synthesized and fully characterized with spectroscopy. Meanwhile,a reasonable multistep continuous reaction mechanism is proposed for this three-component reaction.