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.
梁英
,
贺红武
,
何海峰
,
杨自文
. 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[J]. 有机化学, 2012
, 32(08)
: 1513
-1518
.
DOI: 10.6023/cjoc1201041
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 phos- phonates (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.
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