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[目的]合成6-醚基香豆素衍生物并测试抑菌活性。[方法]邻甲基对苯二酚与乙酰乙酸乙酯经Peachmann缩合得到6-羟基-4,7-二甲基香豆素,随后与取代苄氯无溶剂研磨,合成12个目标化合物4a~4l。[结果]化合物经1H NMR和高分辨质谱鉴定。初步活性试验表明:质量浓度为100 mg/L时,目标化合物对5个靶标真菌有较好的抑菌活性,其中化合物4b、4c和4e对芒果蒂腐病菌的抑制率超过90%。[结论]无溶剂研磨绿色合成了具有较好抑菌活性的6-醚基香豆素衍生物。
[Objective] The research aimed to synthesize 6-ether coumarin derivatives and test their antibacterial activity. [Method] Peachmann condensation of o-methyl hydroquinone and ethyl acetoacetate to give 6-hydroxy-4,7-dimethylcoumarin followed by solvent-free substitution of benzyl chloride to synthesize 12 target compounds 4a ~ 4l. [Result] The compounds were identified by 1H NMR and high resolution mass spectrometry. The preliminary activity test showed that the target compound had good antibacterial activity against five target fungi at a concentration of 100 mg / L, and the inhibitory rates of compounds 4b, 4c and 4e against the pathogen Trichogramma halophila were over 90%. [Conclusion] The 6-ether coumarin derivatives with good bacteriostasis activity were synthesized by solvent-free grinding green.