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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Bibliographic Details
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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Summary: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.
ISSN:1420-3049