Baqi Younis, Müller Christa E
Pharmaceutical Institute, University of Bonn, D-53121 Bonn, Germany.
Org Lett. 2007 Mar 29;9(7):1271-4. doi: 10.1021/ol070102v. Epub 2007 Mar 10.
[structure: see text]. The synthesis of anilinoanthraquinones 3a-z was achieved by a new, Cu(0)-catalyzed, microwave-assisted Ullmann coupling reaction of bromaminic acid (1) with aniline derivatives 2a-z in phosphate buffer. Good to excellent isolated yields were obtained within only 2-20 min at 80-120 degrees C and 40-100 W. The new procedure provides the first general access to anilinoanthraquinones, furnishing a number of previously inaccessible compounds. It is superior to classical methods in all aspects, including yields, reaction time, and versatility.
[结构:见原文]。通过溴氨酸(1)与苯胺衍生物2a - z在磷酸盐缓冲液中进行的新型铜(0)催化、微波辅助乌尔曼偶联反应,实现了苯胺基蒽醌3a - z的合成。在80 - 120℃和40 - 100瓦的条件下,仅需2 - 20分钟就能获得良好至优异的分离产率。该新方法首次为合成苯胺基蒽醌提供了通用途径,制备出了许多以前无法获得的化合物。在产率、反应时间和通用性等所有方面,它都优于传统方法。