6-甲基-4-(3-三氟甲基苯基)-3(2H)-哒嗪酮的合成与生物活性研究

Synthesis and Herbicidal Activity of Novel 6-Methyl-4-(3-trifluoro-methylphenyl)pyridazin-3(2H)-one

在对3-三氟甲基-1,1'-联苯类衍生物类化合物进行CoMFA计算的基础上,设计合成了化合物6-甲基-4-(3-三氟甲基苯基)-3(2H)-哒嗪酮(T-1),分别采用小杯法、浮萍法和盆栽法对其除草活性进行了较详细的研究,发现化合物T-1具有很好的白化活性和除草效果.研究了T-1的合成路线,实施了三条完全不同的路线进行合成,比较了三条路线的优缺点.

6-Methyl-4-（3-trifluoromethylphenyl）pyridazin-3（2H）-one （T-1） was designed and synthesized based on the comparative molecular field analysis （CoMFA） of three series herbicidal 3-trifluoromethyl- 1,1＇-biphenyl derivatives inhibiting phytoene desaturase. Herbicidal activities of T-1 were evaluated through barnyardgrass, rape cup tests, Spirodela polyrrhiza （L.） and greenhouse test. T-1 exhibited good herbicidal and bleaching activites. Herein, we report tThree methods for the preparation of T-1 were reported.