Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leics, LE11 5RH, United Kingdom.
Org Lett. 2010 Mar 19;12(6):1264-7. doi: 10.1021/ol100083w.
A novel, simple synthesis of aryl and heteroaryl acyl sulfamides has been developed via palladium-catalyzed carbonylation of aryl or heteroaryl halides in the presence of sulfamide nucleophiles. A range of reactions illustrating the wide scope of this reaction was carried out under microwave irradiation in a vessel equipped with a gas inlet adapter and proceeded in good to excellent yields.
通过钯催化的芳基或杂芳基卤化物在磺酰胺亲核试剂存在下的羰基化反应,开发了一种新颖、简单的芳基和杂芳基酰基磺酰胺的合成方法。在配备有气体入口适配器的容器中进行了一系列反应,证明了该反应具有广泛的适用范围,在微波辐射下反应收率良好至优秀。