N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯的合成及生物活性研究

Synthesis and Biological Activity of Methyl N-Methoxy-N-[2-(1,6-dihy- dro-1-substituent-6-oxo-pyridazin-3-yloxymethyl)phenl]carbamates

为了寻找高效、低毒的农药,设计合成了一系列新的N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯化合物3a～3k,其结构经IR,1HNMR,LC/MS和元素分析确认.生物活性测定表明,部分化合物在50mg/L下对小麦赤霉病菌(Gibberellazeae)、稻瘟病菌(Pyriculariaoryzae)和黄瓜灰霉病菌(Botrytiscinerea)有较好的抑菌活性.

In an attempt to find novel compounds with high activity and low toxicity, a series of novel methyl N-methoxy-N-[2-(1,6-dihydro-1-substituent-6-oxo-pyridazin-3-yloxymethyl)phenyl]carbamate derivatives 3a similar to 3k were designed and synthesized by bioisoster principle. Their structures were confirmed by (1)H NMR, IR, LUMS spectra and elemental analysis. The preliminary biological activity tests show that some compounds possess fungicidal activities against Pyricularia oryzae, Botrytis cinerea and Erysiphe graminis.