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Updated: May 31, 2025

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Published on: January 3, 2018
The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives
Shuanghui Hua1, Jimin Moon1, Taeho Lee1
1Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of Korea.
Abstract:
A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-d]pyrimidin-7(6H)-one structure was synthesized through efficient Thorpe-Ziegler and cyclization reactions. The thiazolo[4,5-d]pyrimidin-7(6H)-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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