以BF3-Et2O为催化剂一锅多组分合成β-乙酰氨基酮

P. Rawat, P. Rawat, Piyush Kumar
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引用次数: 0

摘要

以不同的酮类1a-1f、醛类2a-2g、乙腈类3a-3d为起始原料,合成了具有生物活性的β-乙酰氨基羰基化合物4a-4h。我们还尝试用苯丙酮和脱氧苯甲酸代替酮合成这些化合物,得到产物4i-4j。给出了H-NMR谱图。在QSAR研究的基础上,对一些化合物在小鼠体内的抗血栓活性进行了测试。化合物4f、4h和4j的保护率较低。
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One-Pot Multicomponent Synthesis of β-Acetamido Ketones Using BF3-Et2O as Catalyst
Starting from different ketones 1a-1f , aldehyde 2a-2g , and acetonitriles 3a-3d we synthesize some bioactive β- Acetamido carbonyl compounds 4a-4h . We also attempted to synthesize these compounds by using phenylacetone and deoxybenzoins in place of ketones to afford the products 4i-4j . 1 H-NMR spectra are presented. On the basis of QSAR studies, some compounds were tested for their anti-thrombotic activity in mice. Compound 4f , 4h and 4j were found to exhibit less percentage protection.
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