{"title":"The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives.","authors":"Shuanghui Hua, Jimin Moon, Taeho Lee","doi":"10.3390/molecules30020430","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":19041,"journal":{"name":"Molecules","volume":"30 2","pages":""},"PeriodicalIF":4.6000,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11767942/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecules","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.3390/molecules30020430","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
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.
期刊介绍：
Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.
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