Wu Xiongyu, Rönn Robert, Gossas Thomas, Larhed Mats
Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, BMC, Box 574, SE-751 23 Uppsala, Sweden.
J Org Chem. 2005 Apr 15;70(8):3094-8. doi: 10.1021/jo050080v.
The development of a robust palladium-catalyzed amidocarbonylation protocol for the preparation of aromatic acyl sulfonamides utilizing high-density microwave heating is described. This synthetic approach employs Mo(CO)(6) as a convenient CO-releasing reagent and allows for the direct preparation of acyl sulfonamides from both aryl iodides and aryl bromides. The reactions can be performed under air, employing only 15 min of microwave irradiation, to produce acyl sulfonamide derivatives in good to excellent yields. To illustrate the usefulness of this method, we reported the synthesis of a novel hepatitis C virus NS3 protease inhibitor.
本文描述了一种利用高密度微波加热制备芳族酰基磺酰胺的稳健钯催化酰胺羰基化方案的开发。这种合成方法采用Mo(CO)₆作为方便的CO释放试剂，并允许从芳基碘化物和芳基溴化物直接制备酰基磺酰胺。反应可以在空气中进行，仅需15分钟的微波辐射，以良好至优异的产率生成酰基磺酰胺衍生物。为了说明该方法的实用性，我们报道了一种新型丙型肝炎病毒NS3蛋白酶抑制剂的合成。
