化学学报 ›› 2002, Vol. 60 ›› Issue (3): 468-474. 上一篇    下一篇

研究论文

5-依维菌素B_(1a)酯的合成和生物活性

廖联安;李正名;方红云;赵卫光;范志金;刘桂龙   

  1. 厦门大学化学系.福建(361005);南开大学元素有机化学研究所.天津(300071)
  • 发布日期:2002-03-15

Synthesis and Bioactivity of 5-Ivermectin B_(1a) Esters

Liao Lianan;Li Zhengming;Fang Hongyun;Zhao Weiguang;Fan Zhijin;Liu Guilong   

  1. Department of Chemistry, Xiamen University. Xianmen(361005);Institute of Elemento-Organic Chemistry, Nankai University.Tianjin (300071)
  • Published:2002-03-15

依维菌素B_(1a)与羧酸在DMAP/DCC体系中直接酯化,得到10个5-IV B_(1a)酯 衍生物,产率66%~82%;它们的化学结构得到IR,~1H NMR, ~(13)c nmr和MS谱的 确证。它们具有良好的杀虫、杀螨活性。

关键词: 酯化, 依维菌素B, 羧酸, 酯化, 红外分光光度法, 质子磁共振谱法, 杀虫剂

Ten 5-Ivermectin B_(1a) ester derivatives were prepared from Ivermectin B_(1a) and carboxylic acids in the systems of DCC/DMAP. Their chemical structures were determined by IR, ~1H NMR, ~(13)C NMR and MS spectra. The preliminary results of bioassay showed that L-1~L- 10 have good insecticidal activities.

Key words: ESTERIFICATION, Ivermectin B, CARBOXYLIC ACID, ESTERIFICATION, IR, 1HNMR, INSECTICIDES

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