Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
J Org Chem. 2010 Feb 19;75(4):1301-4. doi: 10.1021/jo902533p.
A protocol for rapid and efficient Pd/Cu-catalyzed coupling of aryl bromides and iodides to terminal alkynes has been developed with use of 2-(di-tert-butylphosphino)-N-phenylindole (cataCXium PIntB) as ligand in TMEDA and water. The new protocol successfully couples substrates which failed with standard Sonogashira conditions, and enables an efficient general synthetic route to free fatty acid 1 (FFA1) receptor ligands from 3-(4-bromophenyl)propionic acid.
已经开发出一种使用 2-(二-叔丁基膦基)-N-苯基吲哚（cataCXium PIntB）作为配体在 TMEDA 和水中的快速、高效的 Pd/Cu 催化芳基溴化物和碘化物与末端炔烃偶联的协议。该新协议成功地偶联了在标准 Sonogashira 条件下失败的底物，并为从 3-(4-溴苯基)丙酸合成游离脂肪酸 1（FFA1）受体配体提供了一种有效的通用合成途径。
