Department of Chemistry, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, 223-8522, Japan.
Org Lett. 2013 Feb 15;15(4):848-51. doi: 10.1021/ol303534w. Epub 2013 Jan 31.
Benzoxazine-2-one derivatives are important heterocycle structures because of their various pharmaceutical activities, though their synthetic methods had been limited. In some cases, toxic reagents, such as phosgene or carbon monoxide, are required. It was found that a silver catalyst successfully promoted the incorporation of CO(2) into o-alkynylanilines to afford the corresponding benzoxazine-2-ones bearing Z exo-olefin via 6-exo-dig cyclization at the activated C-C triple bond.
苯并恶嗪-2-酮衍生物因其具有多种药物活性而成为重要的杂环结构，但它们的合成方法受到限制。在某些情况下，需要使用有毒试剂，如光气或一氧化碳。研究发现，银催化剂可以成功地促进二氧化碳与邻炔基苯胺的加成反应，通过在活化的 C-C 三键上进行 6-endo-dig 环化反应，得到相应的带有 Z 型 exo-烯烃的苯并恶嗪-2-酮。
