Rajendran Nanthini, Kamaraj Kiruthigadevi, Janakiraman Saranya, Saral Mary, Dixneuf Pierre H, Bheeter Charles Beromeo
Department of Chemistry, School of Advanced Sciences, Vellore of Institute of Technology Vellore-632014 TamilNadu India
University of Rennes, ISCR, UMR CNRS 6226 35000 Rennes France.
RSC Adv. 2023 May 16;13(22):14958-14962. doi: 10.1039/d3ra02637j. eCollection 2023 May 15.
Herein, we report a simple and efficient synthetic approach for direct amidation of esters C(acyl)-O bond cleavage without any additional reagents or catalysts, using only water as a green solvent. Subsequently, the reaction byproduct is recovered and utilized for the next phase of ester synthesis. This method emphasized metal-free, additive-free, and base-free characteristics making it a new, sustainable, and eco-friendly way to realize direct amide bond formation. In addition, the synthesis of the drug molecule diethyltoluamide and the Gram-scale synthesis of a representative amide are demonstrated.
在此，我们报道了一种简单高效的合成方法，用于酯的直接酰胺化反应，即C(酰基)-O键断裂，无需任何额外的试剂或催化剂，仅使用水作为绿色溶剂。随后，反应副产物被回收并用于酯合成的下一阶段。该方法强调无金属、无添加剂和无碱的特性，使其成为实现直接酰胺键形成的一种新的、可持续的和环保的方式。此外，还展示了药物分子二乙甲苯酰胺的合成以及一种代表性酰胺的克级合成。
