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Synthesis of Highly Substituted Imidazole Uracil Containing Molecules via Ugi-4CR and Passerini-3CR.
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2018-02-26 , DOI: 10.1021/acscombsci.7b00145
Rudrakshula Madhavachary 1 , Tryfon Zarganes-Tzitzikas 1 , Pravin Patil 1 , Katarzyna Kurpiewska 2 , Justyna Kalinowska-Tłuścik 2 , Alexander Dömling 1
Affiliation  

The synthesis of uracil/thymine containing tetra/trisubstituted imidazole derivatives was demonstrated using Ugi/Passerini-reaction followed by a postcyclization reaction sequence. The approach enables the one-pot facile construction of diverse compounds in moderate to excellent yields (47-82%). The 5-fluorouracil and 5-methyluracil moieties afford potentially bioactive molecules with drug-like properties. These scaffolds are currently being utilized in the screening deck of the European Lead Factory.

中文翻译:

通过Ugi-4CR和Passerini-3CR合成高度取代的含咪唑尿嘧啶分子。

含有尿嘧啶/胸腺嘧啶的四/三取代的咪唑衍生物的合成已通过Ugi / Passerini反应和随后的环化反应序列进行了证明。该方法可以以一锅的方式轻松构建中度到优异的产率(47-82%)的各种化合物。5-氟尿嘧啶和5-甲基尿嘧啶部分提供具有药物样性质的潜在生物活性分子。这些脚手架目前正在欧洲铅工厂的筛选平台中使用。
更新日期:2018-02-19
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