Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-01-04 , DOI: 10.1016/j.bmcl.2009.12.102 Xuesen Fan , Dong Feng , Yingying Qu , Xinying Zhang , Jianji Wang , Philippe M. Loiseau , Graciela Andrei , Robert Snoeck , Erik De Clercq
A highly practical and efficient preparation of pyrano[3,2-c]pyridone and pyrano[4,3-b]pyran derivatives was developed via an ionic liquid mediated and promoted multi-component reaction of aldehyde (1), 4-hydroxy-pyridin-2(1H)-one or 4-hydroxy-2-pyranone (2), and malononitrile (3). As an application, a series of pyrimidine nucleoside-pyrano[3,2-c]pyridone or pyrano[4,3-b]pyran hybrids were efficiently obtained. These hybrid compounds were evaluated as potential antiviral and antileishmanial agents and showed encouraging biological activities.
中文翻译:
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实用高效合成吡喃并[3,2- c ]吡啶酮,吡喃并[4,3- b ]吡喃及其与核苷的杂化物作为潜在的抗病毒药和抗疟药
通过离子液体介导和促进的醛(1),4-羟基-吡咯烷酮的多组分反应,开发了一种高度实用和有效的吡喃并[3,2- c ]吡啶酮和吡喃并[4,3- b ]吡喃衍生物的制备方法吡啶-2(1 H)-1或4-羟基-2-吡喃酮(2)和丙二腈(3)。作为应用,有效地获得了一系列嘧啶核苷-吡喃并[3,2- c ]吡啶酮或吡喃并[4,3- b ]吡喃杂化物。这些杂合化合物被评估为潜在的抗病毒药和抗疟药,并显示出令人鼓舞的生物学活性。