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Heterocyclization of a Thiouracil Derivative as a Synthetic Entry to Novel Condensed Pyrimidines of Biological Interest
Russian Journal of Organic Chemistry ( IF 0.8 ) Pub Date : 2020-06-26 , DOI: 10.1134/s1070428020050218
W. Shehta , A. M. Abdel Hamid

Abstract

Chlorination of an S-methyl-5-cyano-6-arylthiouracil derivative afforded a chloropyrimidine which underwent aminolysis followed by cyclization to give pyrimidothiazolpyrimidine and imidazopyrimidines. The same thiouracil derivative was also used to prepare oxadiazolopyrimidines, triazolopyrimidines, and pyrimidotriazepines via a diaminopyrimidine and its cyclization with a variety of reagents. Some of the newly synthesized compounds showed a high antibacterial activity against Gram (+ve) and Gram (–ve) bacteria.


中文翻译:

硫脲嘧啶衍生物的杂环化作为生物感兴趣的新型缩合嘧啶的合成入口

摘要

S-甲基-5-氰基-6-芳基硫尿嘧啶衍生物的氯化得到氯嘧啶,对其进行氨解,然后环化,得到嘧啶并噻唑并嘧啶和咪唑并嘧啶。相同的硫氧嘧啶衍生物还用于通过二氨基嘧啶制备恶二唑并嘧啶,三唑并嘧啶和嘧啶并氮杂卓,并用多种试剂环化。一些新合成的化合物对革兰氏(+ ve)和革兰氏(–ve)细菌具有很高的抗菌活性。
更新日期:2020-06-26
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