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Solid‐Phase Synthesis of Tetramic Acid via Resin‐Bound Enol Ethers as a Privileged Scaffold in Drug Discovery
Advanced Synthesis & Catalysis ( IF 5.4 ) Pub Date : 2018-08-02 , DOI: 10.1002/adsc.201800645
Eva Schütznerová 1 , Allen G. Oliver 2 , Adam Přibylka 3 , Viktor Krchňák 2, 3
Affiliation  

This paper reports the practical synthesis of a tetramic acid scaffold on solid phase using simple, commercially available building blocks under mild conditions. Acyclic precursors were assembled on solid phase in four steps, and cyclization was achieved by Wittig olefination. The target compounds contained three points of diversification and allowed for further modifications while still being attached to the resin. Solid‐phase synthesis represents a method of choice, particularly for parallel synthesis, because the intermediates can be isolated simply and quickly by washing the resin beads, which typically takes only minutes.

中文翻译:

通过树脂结合的烯醇醚作为特权支架在药物发现中固相合成四甲酸

本文报道了在温和条件下使用简单的市售结构单元在固相上实际合成四酸支架的方法。无环前体以四个步骤组装在固相上,并通过维蒂希(Wittig)烯烃化反应实现环化。目标化合物包含三个分散点,可以进行进一步修饰,同时仍与树脂连接。固相合成代表了一种选择的方法,特别是对于平行合成而言,因为可以通过洗涤树脂珠子简单,快速地分离中间体,通常只需几分钟。
更新日期:2018-08-02
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