含1, 3, 4-噻二唑的吡啶联吡唑乙酰胺类化合物的合成及除草活性

Synthesis and herbicidal activity of substituted 2-(1-(3-chloropyridin-2-yl)-3, 5-dimethyl-1H-pyrazol-4-yl) acetic acid derivatives containing 1, 3, 4-thiadiazole

摘要: 以乙酰丙酮、溴乙酸乙酯和2，6-二氯吡啶为起始原料，经取代、肼基化、环合、水解、酸化及缩合等反应，得到9个未见文献报道的吡啶联吡唑乙酰基类化合物 B1~B9 。其结构均经核磁共振氢谱和质谱表征。初步生物活性测定表明：在150 g/hm²的处理剂量下，大部分目标化合物表现出一定的除草活性，其中化合物 B2、B3、B6 和 B8 对苘麻Abutilon theophrasti Medicus、反枝苋Amaranthus retroflexus和凹头苋Amaranthus lividus L.生长的抑制率接近100%。

Abstract: Nine novel 2-(1-(3-chloro pyridin-2-yl)-3, 5-dimethyl-1H-pyrazol-4-yl) acetic acid derivatives B1 - B9 were synthesized from acetylacetone, ethyl bromoacetate and 2, 6-dichloropyridine. The synthesis route included a series of reactions such as substitution, alkylation, cyclization, hydrolysis, and acidification condensation. The chemical structures were characterized by ¹H NMR and MS. Preliminary bioassay showed that most of the above compounds displayed herbicidal activities at the concentration of 150 g/hm². The inhibition rates of B2, B3, B6 and B8 against Abutilon theophrasti Medicus, Amaranthus retroflexus and Amaranthus lividus L. were nearly 100%.