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Synthesis of novel pyrimidine and fused pyrimidine derivatives

机译:新型嘧啶和稠合嘧啶衍生物的合成

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4-Amino-2-(benzylthio)-6-(4-methoxyphenyl)pyrimidine-5-carbonitrile (1) was prepared by treatment of s-benzylthiuronium chloride with 2-(4-methoxybenzylidene)malononitrile in ethanolic sodium hydroxide with hydrazine hydrate to afford the hydrazino derivative 2, which was allowed to react with different electrophilic reagents to give the pyrimidine derivatives 3-12. The proclivity of (E)-2-cyano-3-(4-nitrophenyl)acrylamide (13) towards carbon and nitrogen nudeophiles was also investigated. IR, *H NMR and mass spectra for all the synthesized compounds were discussed. All derived compounds were investigated for anti avian influenza (H5N1) virus activity and compared with zanamivir as control drug. All the synthesized compounds didn't possess any antiviral activity.
机译:4-氨基-2-(苄硫基)-6-(4-甲氧基苯基)嘧啶-5-腈(1)是通过在乙醇氢氧化钠中用水合肼将2-(4-甲氧基亚苄基)丙二腈与2-(4-甲氧基亚苄基)丙二腈处理s-苄基硫代氯化铵制备的。得到肼衍生物2,使其与不同的亲电试剂反应,得到嘧啶衍生物3-12。还研究了(E)-2-氰基-3-(4-硝基苯基)丙烯酰胺(13)对碳和氮亲核体的倾向。讨论了所有合成化合物的IR,* H NMR和质谱。研究了所有衍生化合物的抗禽流感(H5N1)病毒活性,并与扎那米韦作为对照药物进行了比较。所有合成的化合物均不具有任何抗病毒活性。

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