Department of Chemistry, Tsinghua University, Beijing 100084, P. R. China.
J Org Chem. 2011 Aug 19;76(16):6832-6. doi: 10.1021/jo200869a. Epub 2011 Jul 27.
In this novel acid-base jointly promoted CuAAC, the combination of CuI/DIPEA/HOAc was developed as a highly efficient catalytic system. The functions of DIPEA and HOAc have been assigned, and HOAc was recognized to accelerate the conversions of the C-Cu bond-containing intermediates and buffer the basicity of DIPEA. As a result, all drawbacks occurring in the popular catalytic system CuI/NR(3) were overcome easily.
在这种新型的酸碱共同促进的铜催化叠氮-炔环加成反应(CuAAC)中,CuI/DIPEA/HOAc 的组合被开发为一种高效的催化体系。DIPEA 和 HOAc 的作用已经被确定,HOAc 被认为可以加速含有 C-Cu 键的中间产物的转化,并缓冲 DIPEA 的碱性。因此,很容易克服了在流行的催化体系 CuI/NR(3)中出现的所有缺点。