5-芳甲氧基苯基吡唑衍生物的合成及除草活性

Synthesis and Herbicidal Activity of 5-Arylmethoxy Phenylpyrazole Derivatives

以4-氯-2-氟-5-甲氧基苯甲醛为原料,经过缩合、闭环、甲基化、醚化等一系列反应合成了具有5-芳甲基苯基吡唑结构的系列新化合物,其结构经过1H NMR,HRMS确定.初步生物活性测试结果表明,部分化合物具有较高的除草活性,特别是4-氯-3-[4-氯-2-氟-5-(4-甲氧基苯甲氧基)苯基]-1-甲基-5-三氟甲基-1H-吡唑,在9.375 g·hm-2剂量下,对苘麻的抑制率达到95%.

A series of novel 5-arylmethoxy phenylpyrazole derivateves are prepared from 4-chloro-2- fluoro-5-methoxybenzaldehyde via a condensation, ring closure, methylation, etc. All these structures are identified by 1H NMR and HRMS techniques. Preliminary bioassay shows that some of the title compounds exhibit good herbicidal activity against the weeds. Especially, 4-cholro-3-[4-chloro-2-fluoro-5-（4-methoxy- benzyloxy）phenyl]-1-methyl-5-trifluoromethyl）-1H-pyrazole shows 95% inhibition to abutilon at the dosage of 9.375 g·hm- 2.