N-取代2-甲基-4-三氟甲基-5-噻唑甲酰胺的合成及杀菌活性

Synthesis and fungicidal activity of N-substituted 2-methyl-4- trifluoromethyl-5-thiazole carboxamides

摘要: 通过2-甲基-4-三氟甲基-5-噻唑甲酰氯与苯胺或氨基吡啶类化合物反应,合成了7 个未见文献报道的N-取代2-甲基-4-三氟甲基-5-噻唑甲酰胺类化合物,其结构均经核磁共振氢谱、红外光谱、高分辨质谱和元素分析的表征和确认。对8种病原菌进行的初步杀菌活性测试结果表明:目标化合物在50 μg/mL下对水稻纹枯病菌 Pellicularia sasakii 的活性最好(抑制率在72.60%～91.78%之间),其中 6a 的抑制率最高。

Abstract: Seven novel 2-methyl-4-trifluoromethyl-thiazole-5-carboxamides were synthesized by reaction of 2-methyl-4-trifluoromethyl-5-thiazole chloride with aniline or amino pyridine derivatives.Their structures were characterized by 1H NMR,IR,HRMS and elemental analysis.The preliminary bioassay showed that the inhibition rate of the title compounds were between 72.60%-91.78% against Pellicularia sasakii under 50 μg/mL,and the fungicidal activity of compound 6a was the highest.