Department of Chemistry, Iowa State University, Ames, Iowa 50011, USA.
Org Lett. 2011 Aug 5;13(15):4136-9. doi: 10.1021/ol2016803. Epub 2011 Jul 11.
A novel, efficient route to biologically and pharmaceutically important o-(dimethylamino)aryl ketones and acridones has been developed starting from readily available 1,1-dimethylhydrazones of aldehydes and o-(trimethylsilyl)aryl triflates. The reaction proceeds under mild conditions, tolerates a wide range of functional groups, and provides the final products in good to excellent yields.
从醛的 1,1-二甲基腙和邻-(三甲基甲硅烷基)芳基三氟甲磺酸酯出发,开发了一种新颖、高效的生物和药物重要的邻-(二甲氨基)芳基酮和吖啶酮的合成路线。该反应在温和条件下进行,可耐受广泛的官能团,并以良好至优异的收率提供最终产物。