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噻唑并嘧啶酮衍生物的简便固相合成

The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives.

作者信息

Hua Shuanghui, Moon Jimin, Lee Taeho

机构信息

Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of Korea.

出版信息

Molecules. 2025 Jan 20;30(2):430. doi: 10.3390/molecules30020430.

Abstract

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

摘要

通过一种简便的固相合成方法开发了一个噻唑并嘧啶酮衍生物库。对于该反应,通过高效的索普-齐格勒反应和环化反应合成了噻唑并[4,5-]嘧啶-7(6)-酮结构。具有三种多样性的噻唑并[4,5-]嘧啶-7(6)-酮衍生物库共有四个合成步骤和57种化合物。此外,每个合成步骤的产率为65-97%,这非常高。所开发的合成方法和化合物将用于通过噻唑衍生物的构效关系寻找具有生物活性的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab3c/11767942/e672e74430fc/molecules-30-00430-g001.jpg

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