CAS: 205650-65-3; Fipronil Desulfinyl

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120068-79-3 120067-83-6 120068-81-7

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fipronil

📜氟虫腈置于双氧水体系中,用 乙醇,水 用作溶剂,化学反应 16.0H,以40%的收率获得氟甲腈
参考文献:氟虫腈杀虫剂及其砜代谢物和脱亚砜基光产物的选择性毒性机理.
标题:氟虫腈杀虫剂及其砜代谢物和脱亚砜基光产物的选择性毒性机理.
摘要:Fipronil是一种具有三氟甲基亚磺酰基取代基的n-苯基吡唑,它引发了第二代杀虫剂,它们作用于γ-氨基丁酸(gaba)受体,从而阻断了氯离子通道.第一代产品包括聚氯环烷烃α-硫丹和林丹.在这项研究中,我们研究了亚砜氟虫腈及其砜代谢物和脱亚砜基光产物相对于它们在体外和离体的靶位相互作用的选择性毒性机制以及在生物素对砜的氟虫腈作用中的重要性.通过从非竞争性阻滞位点置换4'-乙炔基-4-N-[2,3-3H2]丙基双环原苯甲酸酯([3H] Ebob)来测定gaba受体敏感性的差异,似乎是氟虫腈对昆虫(家蝇和果蝇)的毒性比对所检查的脊椎动物(人,狗,小鼠,鸡,鹌鹑和鲑鱼)的毒性大得多.在昆虫中,氟虫腈及其砜和去亚砜基衍生物的ic50平均值为3至12 Nm,而在脊椎动物中,氟虫腈,氟虫腈砜和去甲硫基氟虫腈的ic50平均值分别为1103,175和129 Nm.昆虫相对于脊椎动物的特异性按以下顺序减少
Doi:10.1021/tx980157T

专利信息

专利号:US-6409988-B1
优先权日:1999-07-01
标 题:Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
发明人：DHANOA DALJIT S; MEEGALLA SANATH; DOLLER DARIO; SOLL RICHARD M
权利人:DIMENSIONAL PHARM INC
摘要:The present invention is directed to radiolabeled compounds of Formula I:or salts thereof, whereR1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substitutedC6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen or amino; andR3-R7 are defined in the specification.The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

专利号:US-6545033-B1
优先权日:1999-10-06
标 题:Fused 1-(2,6-dichloro-4-trifluoromethylphenyl)-pyrazoles, the synthesis thereof and the use thereof as pesticides
发明人：DHANOA DALJIT S; MEEGALLA SANATH; SOLL RICHARD M; DOLLER DARIO; SHA DEYOU; LIU RUIPING; SILVER GARY; LEE YU-KAI
权利人:DIMENSIONAL PHARM INC
摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 is amino, hydrogen, alkyl, hydroxy, halo, alkoxy, alkylamino, dialkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, trifluoroalkylsulfinyl, trifluoroalkylsulfonyl, hydroxy, amino, trifluoromethyl, acetylamino, -OSO2R2, -OS(O)R2, -OC(O)R2, -OC(O)NHR2, or -NHC(O)NHR2 where R2 is C1-4 alkyl or optionally substituted aryl;X, Y and Z are each independently (CH)n, (CR3R4)n, S, S(O), or SO2, wherein n is 1-2, R3 and R4 are defined herein;Q is N or C-R6, wherein R6 is fluoro, chloro, bromo, or iodo;R5 is halo, C1-C6 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, C1-C4 alkylamino, C1-C4 dialkylamino, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 trifluoroalkylsulfinyl, C1-C4 trifluoroalkylsulfonyl, hydroxy, amino, or trifluoromethyl; andwith the proviso that only one of X, Y and Z can be S, S(O) or SO2.