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首页> 外文期刊>Nucleosides, nucleotides and nucleic acids >Efficient one-pot, three-component procedure to prepare new α-aminophosphonate and phosphonic acid acyclic nucleosides
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Efficient one-pot, three-component procedure to prepare new α-aminophosphonate and phosphonic acid acyclic nucleosides

机译:高效的一锅三组分法制备新的α-氨基膦酸酯和膦酸无环核苷

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摘要

An efficient one-pot three-component Kabachnik-Fields reaction of aldehydes (acyclic nucleosides), amines (or amino acid), and triethyl phosphite proceeded for the synthesis of amino-phosphonates using natural phosphate coated with iodine (I_2@NP) as a catalyst. The novel a-aminophosphonate and phosphonic acid acyclic nucleosides were tested for their anti-HCV and anti-HIV activities. The molecular docking showed that the non-activity of these compounds could be due to the absence of hydrophobic pharmacophores.
机译:以包覆碘(I_2@NP)的天然磷酸盐为催化剂,对醛(无环核苷)、胺(或氨基酸)和亚磷酸三乙酯进行了高效的一锅三组分Kabachnik-Fields反应,合成了氨基膦酸盐。测试了新型a-氨基膦酸酯和膦酸无环核苷的抗HCV和抗HIV活性。分子对接表明,这些化合物的无活性可能是由于缺乏疏水性药效团。

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