α-(1-苯基-3-三氟甲基-5-氯吡唑-4-甲酰氧基)-α-芳甲基膦酸酯的合成、晶体结构与生物活性

Synthesis, Crystal Structure and Biological Activity of α-(5-Chloro-3-trifluoromethyl-1-phenylpyrazol-4-carbonyloxy)-α-arylmethyl Phosphonates

通过1-苯基-3-三氟甲基-5-氯吡唑-4-甲酰氯(4)与α-羟基芳甲基膦酸酯(6)的缩合反应,合成了14种标题化合物7a～7n.所有化合物的结构均经1H NMR,IR和元素分析进行了表征,并且采用X射线单晶衍射分析方法进一步测定了化合物7j的结构.初步的生物活性测试表明,部分标题化合物具有一定的杀菌和除草活性.

Fourteen novel α-（substituted pyrazol-4-carbonyloxy）-α-arylmethyl phosphonates 7a～7n were synthesized from the intermediates 5-chloro-3-trifluoromethyl-1-phenylpyrazol-4-carbonyl chloride（4） and α-hydroxyl-α-arylmethyl phosphonates（6）.All compounds synthesized were identified by 1H NMR,IR spectra and elemental analysis,and the structure of 7j was further determined by X-ray single crystal diffraction method.The preliminary bioassay indicated that some compounds showed moderate fungicidal and herbicidal activities.