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5-阿维菌素B1a酯的合成及生物活性
引用本文:廖联安,李正名,方红云,赵卫光,陈明德,范志金,刘桂龙. 5-阿维菌素B1a酯的合成及生物活性[J]. 高等学校化学学报, 2002, 23(9): 1709-1714
作者姓名:廖联安  李正名  方红云  赵卫光  陈明德  范志金  刘桂龙
作者单位: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
基金项目:国家高技术研究发展计划(863计划),29832050,
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  生物活性  酯化  DMAP/DCC  
文章编号:0251-0790(2002)09-1709-06
收稿时间:2001-06-18

Synthesis and Bioactivity of 5-Avermectin B1a Esters
LIAO Lian An ,LI Zheng Ming ,FANG Hong Yun ,ZHAO Wei Guang ,CHEN Ming De ,FAN Zhi Jin ,LIU Gui Long. Synthesis and Bioactivity of 5-Avermectin B1a Esters[J]. Chemical Research In Chinese Universities, 2002, 23(9): 1709-1714
Authors:LIAO Lian An   LI Zheng Ming   FANG Hong Yun   ZHAO Wei Guang   CHEN Ming De   FAN Zhi Jin   LIU Gui Long
Affiliation: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
Abstract:Ten 5 Avermectin B 1a ester derivatives were prepared from avermectin B 1a and carboxylic acids in the systems of DCC/DMAP. Their chemical structures were confirmed by IR, 1H NMR, { 13 C 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.
Keywords:Avermectin B 1a  Bioactivity  Esterification  DMAP/DCC
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