Stevens Marc Y, Wieckowski Krzysztof, Wu Peng, Sawant Rajiv T, Odell Luke R
Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala Biomedical Center, Uppsala University, P. O. Box 574, SE-751 23 Uppsala, Sweden.
Org Biomol Chem. 2015 Feb 21;13(7):2044-54. doi: 10.1039/c4ob02417f.
A microwave-assisted, multicomponent protocol for the synthesis of substituted 3,4-dihydroquinazolinones via a novel cascade imine/cyclization/aza-Henry reaction sequence is reported. Starting from o-formyl carbamates, a series of structurally diverse 3,4-dihydroquinazolinones was synthesized via a cyclic iminium ion intermediate in moderate to excellent yields. Notably, the reaction is fast, flexible, simple to perform and tolerates a variety of functional groups.
报道了一种微波辅助的多组分方法,通过新颖的级联亚胺/环化/氮杂-Henry反应序列合成取代的3,4-二氢喹唑啉酮。从邻甲酰氨基甲酸酯开始,通过环状亚胺离子中间体合成了一系列结构多样的3,4-二氢喹唑啉酮,产率中等至优异。值得注意的是,该反应速度快、灵活性高、操作简单且能耐受多种官能团。