Department of Nuclear Medicine, University Hospital Münster , Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany, and Organic Chemistry Institute, University of Münster , Corrensstrasse 40, D-48149 Münster, Germany.
Org Lett. 2013 Jun 21;15(12):2954-7. doi: 10.1021/ol4010454. Epub 2013 Jun 4.
A practical protocol for the one-pot synthesis of various aryl sulfonamides, notably of pyridine-core-substituted 7-azaindolyl sulfonamides, is described. A key step is the well-known bromine-lithium exchange reaction of an aryl bromide with tert-butyllithium (t-BuLi). Differing from the common practice to use 2 or more equiv of organolithium, the exact amount of t-BuLi needed for a sufficient exchange reaction is determined for each aryl bromide in a GC-MS-assisted experiment.
描述了一种用于一锅法合成各种芳基磺酰胺的实用方案，特别是吡啶核取代的 7-氮杂吲哚基磺酰胺。关键步骤是芳基溴与叔丁基锂（t-BuLi）的众所周知的溴-锂交换反应。与通常使用 2 当量或更多当量的有机锂的做法不同，在 GC-MS 辅助实验中确定了每种芳基溴进行充分交换反应所需的 t-BuLi 的精确用量。
