Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, ICSN, CNRS, 91198 Gif-sur-Yvette Cedex, France.
Org Lett. 2013 Jun 7;15(11):2854-7. doi: 10.1021/ol401181a. Epub 2013 May 23.
A new, simple, and efficient procedure for the one-pot Ugi four-component reaction of alcohols instead of aldehydes is described. Using a stoichiometric amount of IBX or only 1-2% of sodium 2-iodobenzenesulfonate in the presence of Oxone, a wide range of primary alcohols were oxidized to the aldehyde that were directly engaged in the Ugi four-component reaction to afford α-acetamidoamides in good to excellent yields.
描述了一种新的、简单且高效的醇替代醛的一锅法 Ugi 四组分反应方法。在 Oxone 的存在下,使用化学计量的 IBX 或仅 1-2%的 2-碘苯磺酸钠,可将多种伯醇氧化成醛,这些醛可直接参与 Ugi 四组分反应,以良好至优异的收率得到α-乙酰氨基酰胺。