The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives

A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-<i>d</i>]pyrimidin-7(6<i>H</i>)-one structure was synthesized through efficient Thorpe–Ziegler and cyclization reactions. The thiazolo[4,...

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Main Authors: Shuanghui Hua, Jimin Moon, Taeho Lee
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/2/430
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author Shuanghui Hua
Jimin Moon
Taeho Lee
author_facet Shuanghui Hua
Jimin Moon
Taeho Lee
author_sort Shuanghui Hua
collection DOAJ
description A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-<i>d</i>]pyrimidin-7(6<i>H</i>)-one structure was synthesized through efficient Thorpe–Ziegler and cyclization reactions. The thiazolo[4,5-<i>d</i>]pyrimidin-7(6<i>H</i>)-one derivative library with a diversity of three had a total of four synthesis steps and 57 compounds. In addition, the yield per synthesis step was 65–97%, which was very high. The developed synthesis method and compounds will be used to find compounds with biological activity through the thiazole derivative structure–activity relationship.
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series Molecules
spelling doaj-art-085a48e1649f46b1a83321f48acdaf282025-01-24T13:44:01ZengMDPI AGMolecules1420-30492025-01-0130243010.3390/molecules30020430The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone DerivativesShuanghui Hua0Jimin Moon1Taeho Lee2Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of KoreaResearch Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of KoreaResearch Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of KoreaA thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-<i>d</i>]pyrimidin-7(6<i>H</i>)-one structure was synthesized through efficient Thorpe–Ziegler and cyclization reactions. The thiazolo[4,5-<i>d</i>]pyrimidin-7(6<i>H</i>)-one derivative library with a diversity of three had a total of four synthesis steps and 57 compounds. In addition, the yield per synthesis step was 65–97%, which was very high. The developed synthesis method and compounds will be used to find compounds with biological activity through the thiazole derivative structure–activity relationship.https://www.mdpi.com/1420-3049/30/2/430thiazolesolid-phase synthesischemical library
spellingShingle Shuanghui Hua
Jimin Moon
Taeho Lee
The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
Molecules
thiazole
solid-phase synthesis
chemical library
title The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
title_full The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
title_fullStr The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
title_full_unstemmed The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
title_short The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
title_sort facile solid phase synthesis of thiazolo pyrimidinone derivatives
topic thiazole
solid-phase synthesis
chemical library
url https://www.mdpi.com/1420-3049/30/2/430
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