Chang Wei-Jin, Liew Sook Yee, Kurz Thomas, Tan Siow-Ping
Department of Physical Science, Faculty of Applied Sciences, Tunku Abdul Rahman University of Management and Technology, 53300 Kuala Lumpur, Malaysia.
Centre for Foundation Studies, University of Malaya, 50603 Kuala Lumpur, Malaysia.
Beilstein J Org Chem. 2025 Mar 14;21:596-600. doi: 10.3762/bjoc.21.46. eCollection 2025.
The hydantoin scaffold is renowned for its wide-ranging biological activities, including antibacterial, antiviral, anticancer, anti-inflammatory, and anticonvulsant effects. In this study, we present an innovative, sustainable approach to synthesizing hydantoins (-) directly from amino acids. This method employs a column chromatography-free, two-step, one-pot microwave-assisted synthesis that delivers hydantoins in yields ranging from 34% to 89%. The protocol demonstrates exceptional functional group tolerance, accommodating phenyl, aliphatic, phenol, alcohol, heterocyclic, and sulfide groups. This scalable, rapid, and eco-friendly strategy offers a promising avenue for the efficient synthesis of hydantoins, aligning with green chemistry principles and expanding the accessibility of these bioactive compounds for pharmaceutical applications.
乙内酰脲支架因其广泛的生物活性而闻名，包括抗菌、抗病毒、抗癌、抗炎和抗惊厥作用。在本研究中，我们提出了一种创新的、可持续的方法，可直接从氨基酸合成乙内酰脲（-）。该方法采用无柱色谱的两步一锅法微波辅助合成，乙内酰脲的产率在34%至89%之间。该方案显示出优异的官能团耐受性，可容纳苯基、脂肪族、酚基、醇基、杂环基和硫醚基。这种可扩展、快速且环保的策略为乙内酰脲的高效合成提供了一条有前景的途径，符合绿色化学原则，并扩大了这些生物活性化合物在药物应用中的可及性。
