Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Dipartimento di Eccellenza L. 232/2016, Edificio Polifunzionale, Università della Calabria, 87036 Rende (CS), Italy.
Department of Health Sciences, Magna Græcia University, Viale Europa, 88100 Germaneto CZ, Italy.
Molecules. 2019 Aug 8;24(16):2885. doi: 10.3390/molecules24162885.
The exploitation and use of alternative synthetic methods, in the face of classical procedures that do not conform to the ethics of green chemistry, represent an ever-present problem in the pharmaceutical industry. The procedures for the synthesis of benzimidazoles have become a focus in synthetic organic chemistry, as they are building blocks of strong interest for the development of compounds with pharmacological activity. Various benzimidazole derivatives exhibit important activities such as antimicrobial, antiviral, anti-inflammatory, and analgesic activities, and some of the already synthesized compounds have found very strong applications in medicine praxis. Here we report a selective and sustainable method for the synthesis of 1,2-disubstituted or 2-substituted benzimidazoles, starting from -phenylenediamine in the presence of different aldehydes. The use of deep eutectic solvent (DES), both as reaction medium and reagent without any external solvent, provides advantages in terms of yields as well as in the work up procedure of the reaction.
面对不符合绿色化学伦理的经典方法，开发和利用替代合成方法是制药行业始终存在的问题。苯并咪唑的合成方法已成为合成有机化学的一个焦点，因为它们是开发具有药理活性化合物的重要构建块。各种苯并咪唑衍生物表现出重要的活性，如抗菌、抗病毒、抗炎和镇痛活性，一些已经合成的化合物在医学实践中已经找到了非常强的应用。在这里，我们报告了一种从 -苯二胺在不同醛存在下合成 1,2-二取代或 2-取代苯并咪唑的选择性和可持续方法。深共晶溶剂 (DES) 既可用作反应介质，也可用作试剂，无需任何外加溶剂，在产率和反应后处理方面都具有优势。
