{"title":"微波辅助合成具有抗菌活性的新型噻唑并嘧啶及嘧啶-噻唑并嘧啶并嘧啶衍生物。","authors":"Ayman M S Youssef, Ahmed M Fouda, Rasha M Faty","doi":"10.1186/s13065-018-0419-0","DOIUrl":null,"url":null,"abstract":"<p><strong>Background and objective: </strong>A series of thiazolopyrimidine derivatives have been synthesized via multicomponent reaction and tested for biological activities. This research aims to develop a new synthetic method of poly fused pyrimidines under microwave irradiation. 6-Amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles reacted with bromomalono-nitrile to give 3,7-diamino-5-aryl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarbonitrile more willingly than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivatives reacted with carbon disulphide to produce 11-aryl-11H-1,2,3,4,7,8,9,10-octahydropyrimido[4″,5″:4',5']thiazolo[3',2'-a]pyrimido[4,5-d]pyrimidine-2,4,8,10-tetrathione. The above mentioned reactions were established by using both conventional methods and microwave-assisted irradiation.</p><p><strong>Conclusion: </strong>This work provides a new method for preparing poly fused pyrimidines. The microwave-assisted technique is preferable due to the yield enhancements attained, time saving, and environmental safety reactions. The newly prepared compounds were verified for their antimicrobial activities. Also, the absorption and emission of some of the prepared compounds were studied.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"50"},"PeriodicalIF":0.0000,"publicationDate":"2018-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0419-0","citationCount":"15","resultStr":"{\"title\":\"Microwave assisted synthesis of some new thiazolopyrimidine and pyrimidothiazolopyrimidopyrimidine derivatives with potential antimicrobial activity.\",\"authors\":\"Ayman M S Youssef, Ahmed M Fouda, Rasha M Faty\",\"doi\":\"10.1186/s13065-018-0419-0\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background and objective: </strong>A series of thiazolopyrimidine derivatives have been synthesized via multicomponent reaction and tested for biological activities. This research aims to develop a new synthetic method of poly fused pyrimidines under microwave irradiation. 6-Amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles reacted with bromomalono-nitrile to give 3,7-diamino-5-aryl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarbonitrile more willingly than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivatives reacted with carbon disulphide to produce 11-aryl-11H-1,2,3,4,7,8,9,10-octahydropyrimido[4″,5″:4',5']thiazolo[3',2'-a]pyrimido[4,5-d]pyrimidine-2,4,8,10-tetrathione. The above mentioned reactions were established by using both conventional methods and microwave-assisted irradiation.</p><p><strong>Conclusion: </strong>This work provides a new method for preparing poly fused pyrimidines. The microwave-assisted technique is preferable due to the yield enhancements attained, time saving, and environmental safety reactions. The newly prepared compounds were verified for their antimicrobial activities. Also, the absorption and emission of some of the prepared compounds were studied.</p>\",\"PeriodicalId\":9842,\"journal\":{\"name\":\"Chemistry Central Journal\",\"volume\":\"12 1\",\"pages\":\"50\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2018-05-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1186/s13065-018-0419-0\",\"citationCount\":\"15\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemistry Central Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1186/s13065-018-0419-0\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"Chemistry\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry Central Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/s13065-018-0419-0","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"Chemistry","Score":null,"Total":0}
引用次数: 15
摘要
背景与目的:通过多组分反应合成了一系列噻唑嘧啶衍生物,并对其生物活性进行了测试。本研究旨在建立一种微波辐射合成聚融合嘧啶的新方法。6-氨基-4-芳基-2-硫氧基-1,2,3,4-四氢嘧啶-5-碳腈与溴单腈反应生成3,7-二氨基-5-芳基- 5h -噻唑[3,2-a]嘧啶-2,6-二腈比异构体7- h -噻唑[3,2-a]嘧啶更容易生成。噻唑嘧啶衍生物与二硫化碳反应生成11-芳基- 11h -1,2,3,4,7,8,9,10-八氢嘧啶[4″,5″:4',5']噻唑[3',2'-a]嘧啶[4,5-d]嘧啶-2,4,8,10-四硫酮。上述反应是用常规方法和微波辅助辐照建立的。结论:本工作为制备聚融合嘧啶提供了新方法。微波辅助技术由于获得的产率提高,节省时间和环境安全反应而更受欢迎。新制备的化合物具有抗菌活性。并对部分化合物的吸收和发射特性进行了研究。
Microwave assisted synthesis of some new thiazolopyrimidine and pyrimidothiazolopyrimidopyrimidine derivatives with potential antimicrobial activity.
Background and objective: A series of thiazolopyrimidine derivatives have been synthesized via multicomponent reaction and tested for biological activities. This research aims to develop a new synthetic method of poly fused pyrimidines under microwave irradiation. 6-Amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles reacted with bromomalono-nitrile to give 3,7-diamino-5-aryl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarbonitrile more willingly than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivatives reacted with carbon disulphide to produce 11-aryl-11H-1,2,3,4,7,8,9,10-octahydropyrimido[4″,5″:4',5']thiazolo[3',2'-a]pyrimido[4,5-d]pyrimidine-2,4,8,10-tetrathione. The above mentioned reactions were established by using both conventional methods and microwave-assisted irradiation.
Conclusion: This work provides a new method for preparing poly fused pyrimidines. The microwave-assisted technique is preferable due to the yield enhancements attained, time saving, and environmental safety reactions. The newly prepared compounds were verified for their antimicrobial activities. Also, the absorption and emission of some of the prepared compounds were studied.
期刊介绍:
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