Picloram oxime ester derivatives, process for their preparation and their use as herbicides

By esterifying and coupling the atrazine nucleus with an aldoxime or ketoxime fragment, a simple and mild atrazine oxime ester derivative was prepared. This solved the problems of low-dose herbicidal activity and insufficient crop safety of atrazine oxime ester derivatives in the prior art, achieving efficient control of broadleaf weeds and safety for monocotyledonous crops, and providing a new herbicide development solution.

CN122404217APending Publication Date: 2026-07-17GUIZHOU UNIV
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Patent Information

Application Number
CN202610870429.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2026-05-15
Filing Date
2026-06-16
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

In the existing technology, the development of oxime ester derivatives for atrazine herbicides lacks a systematic evaluation of low-dose herbicidal activity, broadleaf weed selectivity, and crop safety. Furthermore, existing preparation methods are not applicable to a variety of aldoxime and ketoxime substrates, and the reaction conditions are harsh and the operation is inconvenient.

Method used

By esterifying and coupling the atrazine nucleus with different aldoxime or ketoxime fragments, and using a synthetic route involving carboxyl activation and subsequent coupling, atrazine oxime ester derivatives were prepared. These derivatives are simple to operate and have mild conditions, making them suitable for serial synthesis and post-emergence application to control broadleaf weeds.

Benefits of technology

It achieves high-efficiency suppression of broadleaf weeds at low doses, maintains safety for monocot crops, provides a direction for the development of new herbicides, and reduces research and development costs and time.

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Abstract

本发明公开了一种毒莠定肟酯类衍生物、其制备方法及其在除草中的应用,属于农药化学与除草剂创制技术领域。毒莠定肟酯类衍生物为毒莠定酰基片段与醛肟、酮肟或亚胺酸酯型含肟底物经O‑酰化偶联形成的化合物。该类化合物可通过将毒莠定在有机溶剂中与缩合剂和缚酸剂混合活化后,再与相应肟类底物反应,经后处理和纯化制得。生物活性测定结果表明,所述化合物对多种阔叶杂草具有较好的苗后抑制活性,其中化合物2r和2s在低剂量条件下仍对反枝苋、苘麻、苜蓿和藜等阔叶杂草表现出较高抑制作用,并对玉米和小麦表现出较好的作物安全性。
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