Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water

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. Th...

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Main Authors: Wei-Jin Chang, Sook Yee Liew, Thomas Kurz, Siow-Ping Tan
Format: Article
Language:English
Published: Beilstein-Institut 2025-03-01
Series:Beilstein Journal of Organic Chemistry
Subjects:
Online Access:https://doi.org/10.3762/bjoc.21.46
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author Wei-Jin Chang
Sook Yee Liew
Thomas Kurz
Siow-Ping Tan
author_facet Wei-Jin Chang
Sook Yee Liew
Thomas Kurz
Siow-Ping Tan
author_sort Wei-Jin Chang
collection DOAJ
description 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.
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series Beilstein Journal of Organic Chemistry
spelling doaj-art-1d077a7549b84108b26feb7428f0ed7b2025-08-20T02:08:15ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972025-03-0121159660010.3762/bjoc.21.461860-5397-21-46Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in waterWei-Jin Chang0Sook Yee Liew1Thomas Kurz2Siow-Ping Tan3Department 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 Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany Department of Physical Science, Faculty of Applied Sciences, Tunku Abdul Rahman University of Management and Technology, 53300 Kuala Lumpur, Malaysia 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.https://doi.org/10.3762/bjoc.21.46amino acidshydantoinmicrowave-assistedone-pot reactionurech synthesis
spellingShingle Wei-Jin Chang
Sook Yee Liew
Thomas Kurz
Siow-Ping Tan
Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
Beilstein Journal of Organic Chemistry
amino acids
hydantoin
microwave-assisted
one-pot reaction
urech synthesis
title Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
title_full Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
title_fullStr Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
title_full_unstemmed Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
title_short Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water
title_sort sequential two step one pot microwave assisted urech synthesis of 5 monosubstituted hydantoins from l amino acids in water
topic amino acids
hydantoin
microwave-assisted
one-pot reaction
urech synthesis
url https://doi.org/10.3762/bjoc.21.46
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