Center for Molecular Science and Engineering, College of Sciences, Northeastern University, Shenyang 110819, P. R. China.
Org Biomol Chem. 2020 Nov 7;18(41):8486-8490. doi: 10.1039/d0ob01899f. Epub 2020 Oct 16.
An efficient method for the construction of various pyrazolo[5,1-a]isoquinolines has been achieved via Ru(ii)-catalyzed α-carbonyl sulfoxonium ylide annulations with aryl substituted pyrazoles. This oxidant-free transformation occurred through pyrazole-directed C-H activation, Ru-carbene insertion, and acid-promoted carbonyl condensation processes, enabling dual C-C and C-N bond formation. A broad substrate scope with respect to both coupling components worked efficiently with high yields.
通过 Ru(ii)催化的芳基取代吡唑与α-羰基磺酰亚胺叶立德的环加成反应，实现了各种吡唑并[5,1-a]异喹啉的高效构建。这种无氧化剂的转化是通过吡唑导向的 C-H 活化、Ru-卡宾插入和酸促进的羰基缩合过程实现的，从而能够形成双重 C-C 和 C-N 键。该反应具有广泛的底物范围，对于偶联组分都具有高效性和高产率。
