Twelve novel carane‐3,4‐diol derivatives were designed, synthesized, and evaluated for their herbicidal activities against Lolium multiflorum Lam. and Brassica campestris for the first time. The relationships between the chemical structural factors, including types, the number or the carbon chain length of functional groups, associated with the lipophilicity and the herbicidal activity of the tested compounds were also discussed. The results showed that most of newly synthesized compounds had a dose‐dependent, herbicidal activity against the root and shoot growths of Lolium multiflorum Lam. and Brassica campestris. Compared to carane‐3,4‐diol, most of the target derivatives possessed improved lipophilicity and certain solubilities in representative solvents with different polarities. Particularly, ester derivatives 3a‐3b and 3e can be dissolved or dispersed in water, but also displayed higher herbicidal activity against Lolium multiflorum Lam. and Brassica campestris than other ester derivatives. The 50% inhibitory concentration (IC50) value of compound 3e against shoot growth of Brassica campestris (0.485 mmol/L) was superior to that of commercial herbicide glyphosate (1.14 mmol/L), indicating that the potential application as a water‐based herbicide for Brassica campestris control.

中文翻译：

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Carane-3,4-二醇衍生物作为潜在的水基除草剂

设计、合成了 12 种新型卡烷-3,4-二醇衍生物，并评估了它们对黑麦草的除草活性。和首次发现油菜。还讨论了化学结构因素（包括官能团的类型、数量或碳链长度）与测试化合物的亲脂性和除草活性之间的关系。结果表明，大多数新合成的化合物对黑麦草根和芽的生长具有剂量依赖性的除草活性。和油菜。与carane-3,4-二醇相比，大多数目标衍生物具有改善的亲脂性，并且在不同极性的代表性溶剂中具有一定的溶解度。特别是，酯衍生物3a-3b和3e可以溶解或分散在水中，而且对黑麦草也表现出较高的除草活性。与其他酯衍生物相比，油菜。化合物3e对白菜地上部生长的50%抑制浓度（IC50）值（0.485 mmol/L）优于市售除草剂草甘膦（1.14 mmol/L），表明其作为水基除草剂的潜在应用前景用于控制油菜。