| 夏新宇,梅家乐,查步寒,刘晓晖.羧酸直接酰胺化的催化研究进展[J].分子催化(中英文),2025,39(3):288-296 |
| 羧酸直接酰胺化的催化研究进展 |
| Research Progress in Direct Catalytic Amidation of Carboxylic Acids |
| 投稿时间：2025-03-07 修订日期：2025-03-31 |
| DOI：10.16084/j.issn1001-3555.2025.03.010 |
| 中文关键词: 直接酰胺化 酸催化 羧酸 胺 酰胺 |
| 英文关键词:direct amidation acid catalysis carboxylic acid amine amide |
| 基金项目:国家自然科学基金(22072042)[National Natural Science Foundation of China (22072042)]. |
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| 中文摘要: |
| 酰胺在生物学、药学、化工等领域中具有重要的地位, 其合成方法也是有机合成领域中最为基础且关键的方法之一. 在生物体内, 酰胺键是氨基酸通过酶脱水缩合而成的; 而化学合成时, 酰胺键通常是使用化学计量的偶联剂将羧酸转化为活性更高的酰氯等中间体, 再同胺进行缩合反应, 但这种方法存在原子经济性差、造成环境污染等问题. 相比之下, 羧酸和胺直接脱水合成酰胺的过程在单一官能团参与的理想反应条件下只有副产物水, 原子利用率高, 具有绿色环保和经济性的优势. 本文总结了各种用于羧酸和胺直接酰胺化反应的催化剂, 如硼基催化剂、磷基催化剂、金属催化剂、生物催化剂等, 并分析了当前催化剂可能存在的问题, 为酰胺化合物合成方法的设计与开发提供了一定的思路. |
| 英文摘要: |
| The amide bond occupies a pivotal position in biology, pharmaceutical science, and chemical engineering, with its synthetic methodology constituting one of the most fundamental and critical techniques in organic synthesis. In biological systems, enzymatic dehydration condensation of amino acids orchestrates amide bond formation. Conventional chemical synthesis, however, relies on stoichiometric coupling reagents to convert carboxylic acids into activated intermediates (e.g., acyl chlorides) for subsequent amine condensation. This conventional approach presents inherent drawbacks including suboptimal atom economy and environmentally detrimental reagent waste. In marked contrast, the direct dehydration amidation between carboxylic acids and amines under ideal single-functional-group reaction conditions demonstrates compelling advantages: exclusive generation of water as a byproduct, exceptional atom utilization efficiency, and inherent alignment with green chemistry principles and economic sustainability. This comprehensive review critically evaluates catalytic systems for direct amidation (encompassing boron-based, phosphorus-based, metal-based, and biocatalytic strategies), identifies persistent challenges in catalyst design, and proposes strategic frameworks to guide future innovations in sustainable amide synthesis technology. |
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