School of Chemistry, Main Building, Cardiff University, UK.
Org Lett. 2010 Feb 19;12(4):812-5. doi: 10.1021/ol902885j.
A simple and effective method for the preparation of benzoxazolones from nitroarenes or aryl halides is described. Partial reduction of a nitro group in the presence of a chloroformate followed by a microwave-assisted rearrangement/ring closure sequence provides a convenient and practical procedure to prepare this important pharmacophore. Rearrangement precursors were also accessed from aryl halides through transition-metal-catalyzed coupling.
本文描述了一种从硝基芳烃或芳基卤化物制备苯并恶唑酮的简单有效的方法。在氯甲酸酯存在下部分还原一个硝基，然后进行微波辅助重排/环合反应序列，为制备这一重要药效团提供了一种方便实用的方法。重排前体也可以通过过渡金属催化偶联从芳基卤化物获得。
