4-取代的2-(2-氟-3-三氟甲基苯基)-1,3,4-噁二嗪-5-酮衍生物的合成及其生物活性

The Synthesis and the Bioactivity of 4-Substituted-2-(2-fluoro-3-trifluoromethyl-phenyl)-1,3,4-dioxazin-5-ones

以2-氟-3-三氟甲基苯甲酰肼为起始原料,经与氯乙酰氯酰肼化,然后在碳酸钾的作用下进行环合,得到2-(2-氟-3-三氟甲基苯基)-1,3,4-噁二嗪-5-酮,最后通过与各种卤代烃反应,在4位N上引入不同基团,合成了18个未见报道的2-(2-氟-3-三氟甲基苯基)-1,3,4-噁二嗪-5-酮衍生物。所有化合物通过核磁共振鉴定,生物测试结果表明化合物1～化合物3对瓜类炭疽病具有较好的活性。

Eighteen novel 4-substituted-2-（2-fluoro-3-trifluoromethyl-phenyl）-1,3,4 -dioxazin-5-ones were synthesized by the stating material 2-fluoro-3-trifluoromethyl-benzoic acid hydrazide, which reacted with chloro-acetyl chloride and then with potassium carbonate, and finally reacted with alkenyl halide. All the structures were confirmed by ^1H NMR. The preliminary bioassay showed that the compounds 1,2,3 had good fungicidal activity for Colletotrichura lagenarium.