Department of Chemistry, Tsinghua University, Beijing 100084, People's Republic of China.
J Org Chem. 2010 Oct 15;75(20):7002-5. doi: 10.1021/jo101495k.
In this article, we proved that all three key steps in the catalytic cycle of CuAAC can proceed in the presence of carboxylic acids and the latter two steps can be promoted significantly by carboxylic acids. Benzoic acid showed the best promotion activity, and the acids with strong chelating ability to Cu(I) ion could not serve for this purpose. Thus, the first carboxylic acid-promoted highly efficient CuAAC was established.
在本文中,我们证明了 CuAAC 催化循环中的所有三个关键步骤都可以在羧酸存在的情况下进行,并且后两个步骤可以被羧酸显著促进。苯甲酸表现出最佳的促进活性,而对 Cu(I)离子具有强螯合能力的酸则不能用于此目的。因此,建立了第一个羧酸促进的高效 CuAAC。