摘要
2-溴乙酰芳胺与水杨醇在碳酸钾的作用下经氧烷基化反应合成了一系列新型N-芳基-2-(2-羟基苄氧基)乙酰胺类化合物2,并用1H NMR、13C NMR等对目标化合物的结构进行了表征。测定了化合物2的离体抑菌活性和抗癌活性,结果表明化合物N-(3-甲基苯基)-2-(2-羟基苄氧基)乙酰胺(2c)和N-(4-氯苯基)-2-(2-羟基苄氧基)乙酰胺(2j)对水稻稻瘟病菌的抑制活性均为91.8%,化合物2c对黄瓜灰霉病菌、菌核病菌的抑制活性分别为88.6%和86.7%。化合物N-(2-甲氧基苯基)-2-(2-羟基苄氧基)乙酰胺(2e)、N-(2-氯苯基)-2-(2-羟基苄氧基)乙酰胺(2h)对肝癌细胞HCCLM3的抑制率为94.2%和92.4%。
A series of novel N-aryl-2-(2-hydroxybenzyloxy)acetamides were synthesized by the reaction of N-aryl-2-bromoacetamides with salicyl alcohol in the presence of potassium carbonate.The structures of the target compounds were characterized by 1H NMR and 13C NMR.The in vitro fungicidal and antitumor activity of compounds 2 were evaluated.The results showed that both compounds 2c and 2j exhibited 91.8%activity against Magnaporthe oryzae.Compound 2c also displayed 88.6%and 86.7%activity against Botrytis cinerea and Sclerotinia sclerotiorum,respectively.Compounds 2e and 2h showed 94.2%and 92.4%activity against HCCLM3.
作者
肖湘昭
唐子龙
林迪
陈哲彦
胡在秋
XIAO Xiang-zhao;TANG Zi-long;LIN Di;CHEN Zhe-yan;HU Zai-qiu(Key Laboratory of Theoretical Organic Chemistry and Functional Moleculeof Ministry of Education,Hunan University of Science and Technology,Xiangtan 411201,China;School of Chemistry and Chemical Engineering,Hunan University of Science and Technology,Xiangtan 411201,China)
出处
《精细化工中间体》
CAS
2024年第3期5-9,37,共6页
Fine Chemical Intermediates
基金
国家自然科学基金项目(22277025,21877034)
湖南省自然科学基金项目(2022JJ30240)
湖湘高层次人才聚集工程-创新团队(2021RC5028)。
