A large number of chemicals including surfactants, nootropic drugs and pesticides contain an N-acylated lactam moiety in their molecular structure. In this work, the direct, catalytic N-acylation of a number of lactams with various unactivated carboxylic acids is reported. Several Lewis acid catalysts were evaluated for their activity in the N-acylation of pyroglutamic acid methyl ester with palmitic acid; the highest activities were observed for zirconium-based catalysts. Yields of up to 97% were obtained utilising 10 mol% Zr(propoxide)₄ in mesitylene at reflux temperature, but ZrOCl₂·8H₂O was determined as the most stable catalyst. The substrate scope was investigated and a number of lactam-carboxylic acid combinations were successfully converted into the desired products in 57–97% yield. This method provides an alternative synthetic pathway towards the drug aniracetam, which can be produced in 84% yield. A plausible catalytic mechanism is presented based on kinetic experiments.

包括表面活性剂，促智药物和杀虫剂在内的许多化学品在其分子结构中均包含N-酰化内酰胺部分。在这项工作中，报道了许多内酰胺与各种未活化的羧酸直接催化N-酰化。评价了几种路易斯酸催化剂在焦谷氨酸甲酯与棕榈酸的N-酰化反应中的活性。锆基催化剂的活性最高。在回流温度下，使用10％摩尔％的均三甲苯中的Zr（丙氧化物）₄可获得高达97％的产率，但ZrOCl ₂ ·8H ₂O被确定为最稳定的催化剂。研究了底物的范围，并成功地将许多内酰胺-羧酸组合物以57-97％的产率转化为所需的产品。该方法为药物阿尼西坦提供了另一种合成途径，可以以84％的产率生产。基于动力学实验，提出了合理的催化机理。