Affiliations 

  • 1 Department of Physical Science, Faculty of Applied Sciences, Tunku Abdul Rahman University of Management and Technology, 53300 Kuala Lumpur, Malaysia
  • 2 Centre for Foundation Studies, University of Malaya, 50603 Kuala Lumpur, Malaysia
  • 3 Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany
Beilstein J Org Chem, 2025;21:596-600.
PMID: 40099301 DOI: 10.3762/bjoc.21.46

Abstract

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 (H2a-j) 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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.