摘要
设计合成了一系列结构新颖的嘧啶联吡唑甲酰胺类化合物5a^5o,其结构均经过1H NM R和MS分析确证。初步生物活性测试结果表明:在有效成分150 g/hm2剂量下苗后茎叶喷雾处理时,化合物(R)-N-[1-(4-氯苯基)乙基]-3-二氟甲基-1-(4,6-二甲氧基嘧啶-2-基)-1H-吡唑-4-甲酰胺(5c)、N-[1-(4-氯苯基)乙基]-1-(4,6-二甲氧基嘧啶-2-基)-N-甲基-3-三氟甲基-1H-吡唑-4-甲酰胺(5i)和N-[1-(4-氯苯基)乙基]-1-(4,6-二甲氧基嘧啶-2-基)-3-三氟甲基-1H-吡唑-4-甲酰胺(5k)对繁缕Stellaria media的抑制率高达90%以上;而同样剂量下苗前土壤喷雾处理时,化合物N-[1-(4-氯苯基)乙基]-3-二氟甲基-1-(4,6-二甲氧基嘧啶-2-基)-1H-吡唑-4-甲酰胺(5b)和5c对繁缕的抑制率达100%。该类结构化合物有望作为除草先导化合物进行开发。
A number of novel pyrimidine substituted pyrazolecarboxamides 5a-5o were synthesized, and their structures were confirmed by 1 H NMR and MS analysis. The preliminary herbicidal activity indicated that Stellaria media growth inhibition rate was over 90% for the compounds( R)-N-[1-(4-chlorophenyl ) ethyl ]-3-( difluoromethyl )-1-( 4 , 6-dimethoxypyrimidin-2-yl )-1 H-pyrazole-4-carboxamide ( 5 c ) , N-( 1-( 4-chlorophenyl ) ethyl )-1-( 4 , 6-dimethoxypyrimidin-2-yl )-N-methyl-3-( trifluoromethyl )-1 H-pyrazole-4-carboxamide ( 5 i ) and N-( 1-( 4-chlorophenyl ) ethyl )-1-( 4 , 6-dimethoxypyrimidin-2-yl)-3-( trifluoromethyl )-1 H-pyrazole-4-carboxamide ( 5 k ) by postemergence foliar spray processing at 150 g/hm2; and the compounds N-[ 1-( 4-chlorophenyl ) ethyl ]-3-( difluoromethyl )-1-( 4 , 6-dimethoxy-pyrimidin-2-yl )-1 H-pyrazole-4-carboxamide ( 5 b ) and 5 c showed inhibition rate of 100% against S. media by preemergence soil spray processing at the same dose. Compounds of this structure can be potentially used as lead compounds for herbicide.
出处
《农药学学报》
CAS
CSCD
北大核心
2015年第2期220-224,共5页
Chinese Journal of Pesticide Science
基金
"十二五"国家科技支撑计划项目(2011BAE06B03-01)
关键词
嘧啶联吡唑甲酰胺
合成
除草活性
pyrimidine substituted pyrazolecarboxamides
synthesis
herbicidal activity