2-(溴甲基)-3-取代丙烯酸酯的合成及生物活性研究

Synthesis and Biological Activities of 2-( bromomethyl)-3-substituted Acrylate

以醛、丙烯酸酯为原料,经Baylis-Hillman反应合成2-(羟基)取代丙烯酸酯(化合物BH),再溴化得到13个2-(溴甲基)-3-取代丙烯酸酯(化合物BHB),经1H NM R分析确证结构.生物活性测试结果表明:在600 mg/L测试质量浓度下,所合成的目标化合物对供试靶标朱砂叶螨均有一定的防效,对其他供试靶标无防效,其中2-(溴甲基)-3-(2,4-二氯苯基)丙烯酸乙酯(化合物BHB-3)对朱砂叶螨防效达100%;在25 mg/L的剂量下,所测试的目标化合物对供试靶标均无杀菌活性.

2-( Hydroxyl) substituted acrylate( compound BH) was synthesized by Baylis-Hillman reaction utilizing aldehyde and acrylate as starting materials. Thirteen 2-( bromomethyl)-3-substituted acrylate( compound BHB) were synthesized by bromination of 2-( Hydroxyl) substituted acrylate( compound BH). Their structures were confirmed by 1 H NMR. Evaluation of their biological activities indicated that the target compounds BHB exhibited efficient insecticidal activity control of tetranychus cinnabarinus at 600 mg/L,but had no activity on other test targets, including ethyl 2-( bromomethyl)-3-( 2,4-dichlorophenyl) acrylate( compound BHB-3) showed insecticidal activity with 100 %. The target compounds BHB have not exhibited bactericidal activity against test targets at 25 mg/L.