Laboratory of Applied Chemistry, Heterocycles, Fats and Polymers, Faculty of Science, University of Sfax, 3000 Sfax, Tunisia.
Molecules. 2010 Dec 3;15(12):8841-55. doi: 10.3390/molecules1512884.
In this paper we present the room temperature synthesis of a novel serie of 1,4-disubstituted-1,2,3-triazoles 4a-l by employing the (3+2) cycloaddition reaction of pyrimidinones containing alkyne functions with different model azides in the presence of copper sulphate and sodium ascorbate. To obtain the final triazoles, we also synthesized the major precursors 6-amino-5-cyano-1,4-disubstituted-2(1H)-pyrimidinones 3a-r from ethyl 2,2-dicyanovinylcarbamate derivatives 2a-c and various primary aromatic amines containing an alkyne group. The triazoles were prepared in good to very good yields.
本文通过在硫酸铜和抗坏血酸钠存在下，使含有炔基的嘧啶酮与不同模型叠氮化物进行（3+2）环加成反应，室温合成了一系列新型 1,4-二取代-1,2,3-三唑 4a-l。为了得到最终的三唑，我们还通过乙基 2,2-二氰基乙烯基氨基甲酸酯衍生物 2a-c 和各种含有炔基的芳基伯胺合成了主要前体 6-氨基-5-氰基-1,4-二取代-2(1H)-嘧啶酮 3a-r。三唑的产率良好至非常好。
