Chemical Engineering College, Nanjing University of Science and Technology , Nanjing, 210094, P. R. China.
ACS Comb Sci. 2012 May 14;14(5):309-15. doi: 10.1021/co3000117. Epub 2012 Apr 17.
An efficient copper-free protocol for the synthesis of 5-methyl-1H-1,2,3-triazole-modified peptidomimetics through the combination of Ugi four-component reaction with a three-component cycloaddition, has been developed. The copper-free straightforward process is suitable for drug discovery. The chemoselective preparation of 1,4-disubstituted, triazole-modified peptidomimetics by using alkynyl substituted amines may have potential biological and synthetic application. At last, a "Lapinski type" analysis of the physical properties was performed, which is expected to help drug discovery.
开发了一种通过 Ugi 四组分反应与三组分环加成相结合合成 5-甲基-1H-1,2,3-三唑修饰的肽模拟物的高效无铜协议。无铜直接工艺适用于药物发现。使用炔基取代的胺选择性制备 1,4-二取代、三唑修饰的肽模拟物可能具有潜在的生物和合成应用。最后，对物理性质进行了“Lapinski 型”分析，有望有助于药物发现。
