氟虫腈硫代磷酸酯衍生物的合成及生物活性

Synthesis and Bioactivity of Fipronil Phosphorothioate Derivatives

摘要: 以5-氨基-1-(2,6-二氯-4-三氟甲基苯基)-3-氰基吡唑-4-二硫化物( 1 )为起始原料,经过还原和磷酸酯化反应合成了9个新型氟虫腈硫代磷酸酯衍生物,其结构经红外、核磁共振氢谱和质谱确证。初步的生物活性测定结果表明:在50 mg/L浓度下,所有新化合物对孑孓Culex pipiens pallens 24 h的致死率均为100%。

Abstract: 9 novel fipronil phosphorothioate derivatives were synthesized starting from 5-amino-1-(2,6-dichloro-4-trifluoromethylphenyl)-3-cyanopyrazole-4-disulfide ( 1 ) via reduction and phosphoratation.The structures of all compounds were confirmed by IR,1H NMR,and MS spectra.Preliminary bioassays showed that all new compounds exhibited 100% lethal efficiency against Culex pipiens pallens at 50 mg/L.