Department of Engineering, Carbon Dioxide Activation Center (CADIAC), Interdisciplinary Nanoscience Center (iNANO), Aarhus University, Gustav Wieds Vej 14, DK-8000 Aarhus C, Denmark.
Org Biomol Chem. 2020 Feb 19;18(7):1417-1425. doi: 10.1039/c9ob02635e.
A copper-catalyzed decarboxylative trifluoromethylation of (hetero)aromatic iodides has been developed. Importantly, this new copper-catalyzed reaction operates in the absence of any ligands and metal additives. The protocol shows good functional group tolerance and is compatible with heteroaromatic systems. The reaction proved scalable to a 15 mmol scale with increased yield. Finally, late-stage installation of the trifluoromethyl functionality afforded the N-trifluoroacetamide variant of the antidepressant agent, Prozac, demonstrating the applicability of the developed method.
一种铜催化的(杂)芳基碘代物的脱羧三氟甲基化反应已经被开发出来。重要的是,这种新的铜催化反应在没有任何配体和金属添加剂的情况下进行。该方案显示出良好的官能团耐受性,并且与杂芳环体系兼容。该反应可在 15 mmol 规模下放大,产率提高。最后,通过后期安装三氟甲基官能团,得到了抗抑郁药百忧解的 N-三氟乙酰胺变体,证明了所开发方法的适用性。