Division of Applied Chemistry, Institute of Engineering, Tokyo University of Agriculture and Technology, Koganei, Tokyo 184-8588, Japan.
Org Lett. 2013 Jun 7;15(11):2672-5. doi: 10.1021/ol4009816. Epub 2013 May 22.
The metal-free [2 + 2 + 1] annulation of alkynes, nitriles, and O-atoms for the regioselective assembly of 2,4-disubstituted and 2,4,5-trisubstituted oxazole compounds has been achieved by the use of PhIO with TfOH or Tf2NH. The present reaction could be applied to a facile synthesis of an anti-inflammatory drug.
通过使用 PhIO 与 TfOH 或 Tf2NH,实现了炔烃、腈和 O-原子的无金属[2+2+1]环化反应,用于区域选择性地组装 2,4-二取代和 2,4,5-三取代恶唑化合物。本反应可应用于抗炎药物的简便合成。