【摘要】 以四氢芳樟醇为原料，设计合成了17种四氢芳樟基酰胺类化合物（2,4a～4p）,得率64.8%～96.9%。通过FT-IR、¹H NMR、¹³C NMR和HRMS表征了系列化合物的结构，并评价了目标化合物对黑麦草和稗草的除草活性。研究结果表明：四氢芳樟基酰胺类化合物对黑麦草和稗草均有一定的生长抑制活性，化合物2、4a、4o对黑麦草的萌芽前（芽前）除草活性最好，对黑麦草根长的半数抑制浓度(IC₅₀)值分别为0.05、 0.05和0.03 mmol/L（稍差于阳性对照草甘膦）,对黑麦草茎长的IC₅₀值分别为0.06、 0.05和0.05 mmol/L（优于草甘膦）。化合物4b对稗草根长和茎长的IC₅₀值分别为0.06和0.15 mmol/L（与草甘膦相同）。构效关系分析表明：四氢芳樟基酰胺类化合物在不同杂草间具有选择性；含烷基取代的化合物除草活性强于含苯环和呋喃环的，苯环上含给电子基团时活性强于含吸电子基团的，且给电子基团位于苯环邻位和间位时除草活性更好。更多还原

【Abstract】 Seventeen tetrahydrolinalyl amides（2, 4a-4p） were designed and synthesized using tetrahydrolinalool as starting material. Their structures were characterized by FT-IR, ¹H NMR, ¹³C NMR and HRMS, then the herbicidal activities against Lolium perenne and Echinochloa crusgalli were evaluated. The results showed that the tetrahydrolinalyl amides exhibited certain growth inhibitory effects on L. perenne and E. crusgalli. Compounds 2, 4a, 4o showed the best pre-emergence herbicidal activity against L. perenne, where the inhibitory concentration 50%(IC₅₀) values for the root growth of L. perenne were 0.05, 0.05, and 0.04 mmol/L, respectively（weaker than that of the positive control glyphosate）, and the IC₅₀ values for the shoot of L. perenne were 0.06, 0.05, and 0.05 mmol/L, respectively（stronger than that of glyphosate）. The IC₅₀ values of compound 4b on root and shoot growth of E. crusgalli were 0.06 and 0.15 mmol/L（equal to that of glyphosate）, respectively. The structure-activity relationship analysis showed that tetrahydrolinayl amides exhibited selectivity among different weed species. The compounds containing alkyl group showed higher herbicidal activity than that of benzene ring and furan ring. The herbicidal activity of compounds with electron-donating group on benzene ring was stronger than that with electron-withdrawing group, exhibiting better activity when it was located at the ortho-and meta-position of benzene ring.更多还原