A multicomponent cascade cyclization reaction using aryl methyl ketones, aryl amines, and enaminamide reagents to construct 3‐hydroxy‐1H‐pyrrolo[3,4‐b]quinolin‐1‐one skeleton with good substrate compatibility (50 examples) has been reported. The one‐pot, metal‐free process formed two C‐C bonds, two C‐N bonds, and a tetrasubstituted carbon stereocenter containing a hydroxyl group. The reaction enabled modified transformation of drug molecules and derivatization of products.

中文翻译：

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烯酰胺一锅法合成 3-羟基-1H-吡咯并[3,4-b]喹啉-1-酮


据报道，使用芳基甲基酮、芳基胺和烯酰胺试剂构建具有良好底物相容性的3-羟基-1H-吡咯并[3,4-b]喹啉-1-酮骨架的多组分级联环化反应（50个实例）。一锅法、无金属过程形成了两个 C-C 键、两个 C-N 键和一个含有羟基的四取代碳立构中心。该反应实现了药物分子的修饰转化和产物的衍生化。