An efficient protocol for the direct synthesis of 8-arylated tetrahydroquinolines via Pd-catalyzed ortho-arylation of aryl ureas with aryl iodides was developed. The reaction proceeded smoothly in water under ligand-free and surfactant-free conditions, providing the desired products in high yields with remarkable functional group tolerance.
开发了一种高效的协议,通过
钯催化的芳基
脲与芳基
碘的邻位芳基化反应,直接合成8-芳基化的
四氢喹啉。该反应在无
配体和无表面活性剂的
水相条件下顺利进行,以高产率提供了所需产物,并具有显著的官能团耐受性。