Department of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
Molecules. 2020 Oct 12;25(20):4634. doi: 10.3390/molecules25204634.
Alkylamino coupling reactions at the C4 positions of 4-halo-1-1-tritylpyrazoles were investigated using palladium or copper catalysts. The Pd(dba) catalyzed C-N coupling reaction of aryl- or alkylamines, lacking a β-hydrogen atom, proceeded smoothly using BuDavePhos as a ligand. As a substrate, 4-Bromo-1-tritylpyrazole was more effective than 4-iodo or chloro-1-tritylpyrazoles. Meanwhile, the CuI mediated C-N coupling reactions of 4-iodo-1-1-tritylpyrazole were effective for alkylamines possessing a β-hydrogen atom.
研究了钯或铜催化剂作用下 4-卤代-1-三苯甲基吡唑在 C4 位的烷氨基偶联反应。当以 BuDavePhos 作为配体时，Pd(dba) 催化缺乏β-氢原子的芳基或烷基胺的 C-N 偶联反应可以顺利进行。作为底物，4-溴-1-三苯甲基吡唑比 4-碘代或氯代-1-三苯甲基吡唑更有效。同时，CuI 介导的 4-碘代-1-三苯甲基吡唑与具有β-氢原子的烷基胺的 C-N 偶联反应也是有效的。
