Alkoxy‐5‐nitrosopyrimidines: Useful Building Block for the Generation of Biologically Active Compounds

Alkoxy‐5‐nitrosopyrimidines: Useful Building Block for the Generation of Biologically Active Compounds
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烷氧基-5-亚硝基嘧啶:用于生成生物活性化合物的有用构件

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发表时间:
2010
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通讯作者:
M. Melguizo
M. Melguizo
中科院分区:
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文献类型:
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作者:
A. Marchal;M. Nogueras;Adolfo Sánchez;J. N. Low;L. Naesens;E. Clercq;M. Melguizo

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合成了几种烷氧基-5-亚硝基嘧啶,并观察到2-氨基-4,6-二甲氧基-5-亚硝基嘧啶中甲氧基的高区域选择性和连续的亲核芳香取代反应。该方法被应用到有价值的多官能化氨基嘧啶的合成能够模仿融合杂双环衍生物的生物利益。此外,新的化合物作为抗病毒药物进行了评价,并证明了它们作为合成中间体的有用性。
Several alkoxy-5-nitrosopyrimidines were synthesised and high regioselective and sequential nucleophilic aromatic substitution of methoxy groups in 2-amino-4,6-dimethoxy-5-nitrosopyrimidine was observed. The approach was applied to the synthesis of valuable polyfunctionalised aminopyrimidines capable of mimicking fused heterobicyclic derivatives of biological interest. In addition, new compounds were evaluated as antivirals and their usefulness as synthetic intermediates was demonstrated.