吡啶衍生物研究(Ⅷ):2-[(2-氯吡啶)-4-基]-5-烷氨基-1,3,4-噻二唑的合成及其除草活性

Study on pyridine derivatives (Ⅷ): Synthesis and herbicidal activity of 2-(2-chloropyrid-4-yl)-5-alkylamino-1,3,4-thiodiazoles

为寻找新的农药先导化合物 ,依据活性亚结构拼接原理 ,以异烟酸为起始原料 ,共合成了 12个标题化合物 ,其结构通过元素分析、1H和13 CNMR予以确认。所有化合物均具有一定的除草活性 ,且茎叶处理高于土壤处理 ,其中Ⅰ 0 4和Ⅰ 0 6在 1 5kg·hm-2 剂量下 ,茎叶处理对反枝苋、稗草、油菜和苜蓿的抑制率分别达 71 9%～89 2 %和 4 5 3%～ 87 0 % ;因此 。

In the course of continuous researches on pyridine derivatives, twelve 2-(2-chloropyrid-4-yl)-5-alkylamino-1,3,4-thiodiazoles were designed and synthesized. Their structures were confirmed by elemental analysis, 1H and 13 C NMR. All of them give considerable inhibition to tested herbs in preliminary herbicidal screening and foliar treatment is preferable to soil treatment. In foliar model and a dose of 1.5?kg·hm -2 , Ⅰ-04 and Ⅰ-06 gives a 71.9%-89.2% and 45.3%-87.0% inhibition ratio to Amaranthus retroflexus L., Echinochloa crus-galli (L.) Beauv., Brassica campestris var. Oleifera and Medicago sative, respectively. And it proved they are valuable herbicidal lead compounds.