Andrii I. Kysil, A. Biitseva, O. Bugera, T. Yegorova, Z. Voitenko
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引用次数: 0
摘要
介绍了2-(1,2,4-恶二唑-5-基)-2,3-二氢-4- h -铬-4-酮的简单高效合成方法。该方法依赖于cdi介导的取代4-氧-2-羧酸和偕胺肟的环缩合反应。该方案允许制备两种药物载体(2,3-二氢- 4h -铬-4- 1和1,2,4-恶二唑)修饰的2-恶二唑酮，这两种药物在药物发现中需求量很大。
Synthesis of 2-(1,2,4-oxadiazol-5-yl)-2,3-dihydro-4H-chromen-4-ones
Simple and efficient synthesis of 2-(1,2,4-oxadiazol-5-yl)-2,3-dihydro-4H-chromen-4-ones is elaborated. The method relies on CDI-mediated cyclocondensation of substituted 4-oxochromane-2-carboxylic acids and amidoximes. The protocol allows the preparation of 2-oxadiazolylchromanones decorated with two pharmacophores (2,3-dihydro-4H-chromen-4-one and 1,2,4-oxadiazole) that are in high demand in drug discovery.
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