高等学校化学学报 ›› 2002, Vol. 23 ›› Issue (9): 1709.

• 研究论文 • 上一篇    下一篇

5-阿维菌素B1a酯的合成及生物活性

廖联安1, 李正名2, 方红云1, 赵卫光2, 陈明德1, 范志金2, 刘桂龙2   

  1. 1. 厦门大学化学系, 厦门 361005;
    2. 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津 300071
  • 收稿日期:2001-06-18 出版日期:2002-09-24 发布日期:2002-09-24
  • 通讯作者: 李正名(1931年出生),男,教授,博士生导师,工程院院士,从事有机化学、农药化学领域研究工作.E-mail:zml@tjlink.tist.iac.cn E-mail:zml@tjlink.tist.iac.cn
  • 基金资助:

    国家自然科学重点基金(批准号:29832050)资助

Synthesis and Bioactivity of 5-Avermectin B1a Esters

LIAO Lian-An1, LI Zheng-Ming2, FANG Hong-Yun1, ZHAO Wei-Guang2, CHEN Ming-De1, FAN Zhi-Jin2, LIU Gui-Long2   

  1. 1. Depa rtment of Chemistry, Xiamen University, Xiamen 361005, China;
    2. Instituteof Emento-organic Chemistry, State Key Laboratoryof Elemento-Organic Chemistry, Nanka i University, Tianjin 300071, China
  • Received:2001-06-18 Online:2002-09-24 Published:2002-09-24

摘要: 阿维菌素B1a(AVB1a)与羧酸在DMAP/DCC体系中直接酯化,得到10个5-AVB1a酯衍生物,产率50%~79%;其化学结构由IR,1H NMR,13CNMR和MS谱确证.生物活性测定结果表明,部分5-阿维菌素B1a酯衍生物具有良好的杀虫、杀螨活性.

关键词: 5-阿维菌素B1a酯, 生物活性, 酯化, DMAP/DCC

Abstract: Ten 5-Avermectin B1a ester derivatives were prepared from avermectin B1a and carboxylic acids in the systems of DCC/DMAP. Their chemical structures were confirmed by IR, 1H NMR, 13C NMR and MS. Their insecticidal activity was evaluated against Aphis gossypii Glover and Tetranychus truncatus Ehara. It was found that some compounds showed a higher insecticidal activity than Avermectin.

Key words: Avermectin B1a, Bioactivity, Esterification, DMAP/DCC

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