高等学校化学学报

高等学校化学学报 ›› 2011, Vol. 32 ›› Issue (1): 79.

• 研究论文 • 上一篇    下一篇

α-取代苯乙酰胺类化合物的合成及生物活性

李欢欢,王振军,王力钟,李正名,赵卫光   

  1. 南开大学元素有机化学国家重点实验室, 农药国家工程研究中心, 天津300071
  • 收稿日期:2010-03-12 修回日期:2010-05-19 出版日期:2011-01-10 发布日期:2010-12-11
  • 通讯作者: 赵卫光 E-mail:zwg@nankai.edu.cn;zhaoweiguang@foxmail.com
  • 基金资助:

    国家“九七三”计划项目(批准号:  2010CB126105)\, 国家科技支撑计划项目(批准号: 2011BAE06B05\|3)和国家自然科学基金(批准号:  20772069)资助.

Syntheses and Biological Activities of α-Substitued Phenylethyl Amide Compounds

LI Huan-Huan, WANG Zhen-Jun, WANG Li-Zhong, LI Zheng-Ming, ZHAO Wei-Guang*   

  1. State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center, Nankai University, Tianjin 300071, China
  • Received:2010-03-12 Revised:2010-05-19 Online:2011-01-10 Published:2010-12-11
  • Contact: ZHAO Wei-Guang E-mail:zwg@nankai.edu.cn;zhaoweiguang@foxmail.com
  • Supported by:

    National Natural Science Foundation of China

PDF (PC)

摘要： 以香草醛和扁桃酸为原料，经过取代、还原等多步反应，得到N-(取代苄氧基)-α-烷氧基苯乙酰胺类化合物及α-苄胺基苯乙酰胺类两类化合物，其化学结构经过1HNMR，高分辨确认。生物活性测定表明部分化合物对黄瓜霜霉和辣椒疫霉表现出了良好的杀菌活性，如N-(3-甲氧基-4-乙氧基苄氧基)-α-乙氧基-4-氯苯乙酰胺在200μg/mL浓度下对黄瓜霜霉病的防效达到了90%，N-(3-甲氧基-4-乙氧基苄氧基)-α-异丙氧基-4-氯苯乙酰胺在20ug/mL浓度下对辣椒疫霉病的防效达到了80%.

关键词: 苯乙酰胺, 扁桃酰胺, 合成, 杀菌活性

Abstract: Mandipropamid is the first mandelamide fungicide on the market. Two series of novel N-substitued benzyloxy-α-alkoxy phenylacetamide compounds and α-subsitued benzylamino-phenylacetamide compounds, the bioisosteric analogues of Mandipropamid, have been synthesized from Vanillin and mandelic acid by substitution, reduction and so on. Their structures were characterized and determined by 1H NMR, HRMS. The result of the preliminary biological activity tests showed that some of the compounds exhibited some anti-fungal activities. For example, N-(3-methoxyl-4-ethoxylbenzyloxy)-α-ethoxyl-4-chloride-phenylacetamide had inhibition rate 90% against fungicidal activity at the concentration of 200 ug /mL. N-(3-methoxyl-4-ethoxylbenzyloxy)-α-isopropoxy-4-chloride-phenylacetamide had inhibition rate 80% against phytophthora capsici at the concentration of 20 ug /mL.

Key words: Phenylacetamide, Mandelamide, Synthesis, fungicide

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