A Quick Synthesis of 1-Arylpyrrolopyrazinones from Linear Alkynylamide Derivatives
作者:Imanol Tellitu、Esther Domínguez、Leticia Pardo
DOI:10.1055/s-0029-1219218
日期:2010.3
protecting group, the free amino group is used to accomplish a second heterocyclization process onto the newly formed carbonyl group. By appropriate manipulation of these protecting groups and selection of reaction conditions, a series of pyrrolopyrazinones can be obtained in different stages of hydrogenation. hypervalent iodine - alkynylamides - reductive aminations - pyrazinones - bicyclic compounds
提出了一种快速合成吡咯并吡嗪酮衍生物的方法,该方法基于在适当取代的底物的三键上进行正式的双加成。关键的环化步骤的特征是由[双(三氟乙酰氧基)碘]苯(PIFA)介导,由适当官能化的N-保护的N-(氨基乙基)酰胺形成5-芳基吡咯烷酮核。除去保护基后,使用游离氨基在新形成的羰基上完成第二个杂环化过程。通过适当地控制这些保护基并选择反应条件,可以在氢化的不同阶段获得一系列吡咯并吡嗪酮。 高价碘-炔酰胺-还原胺化-吡嗪酮-双环化合物