报道了一种通过邻醛基苯甲酸甲酯的胺化还原/内酰胺化一锅法合成N-取代异吲哚-1-酮的高效方法. 反应包括以NaBH₃CN为还原剂, 邻醛基苯甲酸甲酯与伯芳基胺或烷基胺的胺化还原以及N原子对羰基碳的分子内亲核进攻过程. 对于4-取代芳胺、烷基胺和邻甲基苯胺, 该反应可以在室温下的二氯乙烷中顺利完成转化. 而其他的2-取代芳胺, 则需K₂CO₃ (2 equiv.)促进下在乙腈中回流8 h完成. 该反应的底物适用范围很广, 最高收率可达99%.

An efficient, one-pot synthesis of N-substituted isoindolin-1-ones by an aminative reduction/lactamisation sequence of methyl 2-formylbenzoate is introduced. The reaction process includes aminative reduction of o-phthalaldehydic acid methylesters with primary aryl or alkyl amines using NaBH₃CN and the following intramolecular nucleophilic N-attack on carbonyl carbon atom. For 4-substituted aromatic amines, alkyl amines and o-methylaniline, the transformation can be successfully completed in 1,2-dichloroethane at room temperature. For other 2-substituted aromatic amines, reflux in acetonitrile for 8 h in the presence of K₂CO₃ (2 equiv.) is needed. The reaction scopes were quite broad and up to 96% yield of diverse products was achieved.