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Position: Home > Articles > Synthesis with Solvent-free and Antifungal Activities of 6- Ether Coumarin Derivatives Agrochemicals 2015,54 (10) 724-726+743

无溶剂研磨法合成6-醚基香豆素衍生物及其抑菌活性

作  者:
雷震霖;谢颖;侯文成;骆焱平
单  位:
海南大学环境与植物保护学院
关键词:
6-醚基香豆素;无溶剂;研磨法;抑菌活性
摘  要:
[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。
译  名:
Synthesis with Solvent-free and Antifungal Activities of 6- Ether Coumarin Derivatives
作  者:
LEI Zhen-lin;XIE Ying;HOU Wen-cheng;LUO Yan-ping;College of Environment and Plant Protection, Hainan University;
关键词:
6-ether coumarin derivatives;;solvent-free;;grinding methods;;antifungal activities
摘  要:
[Aims] The purpose is to prepare 6-ether coumarin derivatives and to obtain its antifungal activities.[Methods] 2-Methyl-4-benzenediol was reacted with ethyl acetoacetate via Pechmann condensation to yield6-hydroxy-4,7-dimethyl-coumarin, then the coumarin grinded with substituted benzyl chloride without solvent to yield twelve title compounds 4a-4l. [Results] The structure of the compounds were confirmed by 1H NMR and LC-MS. The preliminary bioassay indicated some compounds, such as 4b, 4c and 4e, displayed over 90% antifungal activities against Botryodiplodia theobromae at 100 mg/L. [Conclusions] 6- Ether coumarin derivatives are green synthesis process under solvent-free, and these title compounds show excellent antifungal activities.
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