5-阿维菌素B_(1a)酯的合成及生物活性

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

阿维菌素 B1 a(AVB1 a)与羧酸在 DMAP/DCC体系中直接酯化 ,得到 1 0个 5 -AVB1 a酯衍生物 ,产率5 0 %～ 79% ;其化学结构由 IR,1 H NMR,1 3C NMR和 MS谱确证 .生物活性测定结果表明 ,部分 5 -阿维菌素 B1 a酯衍生物具有良好的杀虫。

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.