新型含吡唑三嗪类氟化融合杂多环氮抗菌剂的合成——ⅰ

L. Taib, Sofiyah A. Adibani
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引用次数: 3

摘要

本文推导了一种新的含吡唑三嗪基团(5,8,11)的新型氟化融合杂多环氮体系的合成方法:先用二氧基膦、碳酸二乙酯和/或草酸二乙酯在四氢呋喃中环化2-氨基硫代羰基-5-芳基基-3-苯基-1,2,4-三嗪-6(1H) 1(2),再用乙氧基/哌啶环化芳基磺酸肼,最后用醋酸三氟乙酯氟化。通过元素分析和光谱测量,确定了产物的结构。对这些靶点的抗菌活性也进行了评价。
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Synthesis of New Fluorinated Fused Heteropolycyclic Nitrogen Systems Containing a Pyrazolotriazine Moiety as Antimicrobial Agents Part I
A simple route to synthesize novel fluorinated fused hetero-polycyclic nitrogen systems containing a pyrazolotriazine moiety (5,8,11) have been deduced from cyclization of 2-aminothiocarbonyl-5-arylidene-3-phenyl-1,2,4-triazin-6(1H)one (2) with diethoxy-phosphine, diethyl carbonate and/or diethyl oxalate in boil THF followed by cyclo condensation with aryl sulfonic acid hydrazide in EtOH/piperidine and finally fluorination with trifluoroethyl acetate. Structures of the products have been established from their elemental analysis and spectral measurements. The antimicrobial activity of the targets has also been evaluated.
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