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通过母体化合物4-氨基吡啶(4-AP)与N-二异丙基磷酰化氨基酸(DiPP-AA)在Ph3P和C2Cl6体系下的缩合反应,将具有生物活性的氨基吡啶环引入到磷酸化氨基酸结构中,设计、合成了5个N-二异丙基磷酰化氨基酸-N-4-氨基吡啶衍生物A1～A5.所有目标化合物均经IR,1H NMR,13C NMR,31P NMR,MS的表征.初步生物活性测试结果表明:目标化合物对河豚毒素(TTX)中毒的小鼠均有一定的解毒作用,并不同程度地延长了生存时间,而且毒性比母体化合物降低了.
The biologically active aminopyridine ring was introduced to phosphorylation by the condensation reaction of the parent compound 4-aminopyridine (4-AP) and N-diisopropylphosphorylated amino acid (DiPP-AA) under Ph3P and C2Cl6 systems Amino acid structure, five N-diisopropylphosphorylamino-N-4-aminopyridine derivatives A1 ~ A5 were designed and synthesized.All the target compounds were characterized by IR, 1H NMR, 13C NMR, 31P NMR, MS The preliminary bioassay results showed that the target compounds had certain detoxification effects on mice poisoned by tetrodotoxin (TTX), prolonged the survival time to a certain extent and the toxicity was lower than that of the parent compound.