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Efficient Synthesis of Boron-Containing α-Acyloxyamide Analogs via Microwave Irradiation

机译:微波辐射有效合成含硼α-酰氧基酰胺类似物

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In this report, a Passerini three-component reaction utilizing boron-containing carboxylic acids or aldehydes is discussed. The reaction was carried out in water and facilitated by the use of microwave irradiation. This methodology allowed for the efficient formation of a broad range of boron-containing α-acyloxyamides under mild conditions within a short time. Two series of boron-containing α-acyloxyamides were synthesized and subsequently screened for cytotoxicity using the MTT cell viability assay. Two potential lead compounds were found to have potent activity against the HepG2 cancer cell line, demonstrating the potential of this methodology for use in the development of novel pharmaceuticals.
机译:在该报告中,讨论了一种使用含硼羧酸或醛的帕塞里尼三组分反应。反应在水中进行,并通过使用微波辐照促进。这种方法可以在短时间内在温和条件下有效地形成各种含硼的α-酰氧基酰胺。合成了两个系列的含硼α-酰氧基酰胺,随后使用MTT细胞活力测定筛选了细胞毒性。发现两种潜在的先导化合物对HepG2癌细胞系具有有效的活性,证明了这种方法在开发新型药物中的潜力。

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