Herbicidal Phenyltriazolinones Low Application Rates
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Solution Overview
Problem
Existing herbicides based on phenyltriazolinones have unsatisfactory herbicidal properties against harmful plants, particularly at low application rates, and are not adequately compatible with crop plants for commercial use.
Innovation Solution
Development of phenyltriazolinones with specific structural modifications, including varying substituents and attachments, to enhance herbicidal activity while ensuring compatibility with crop plants, including their use in agriculturally suitable salts and compositions with auxiliaries and safeners.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing phenyltriazolinone herbicides are used, then herbicidal action is achieved, but herbicidal activity is insufficient particularly at low application rates
Solution Approach 1:
The patent applies parameter changes by systematically varying substituents at multiple positions (R1-R7, n, Q, W, X, Y, Z) of the phenyltriazolinone core structure to optimize herbicidal activity. Specific substitutions such as introducing electron-withdrawing groups at R4-R6 positions and modifying the triazolinone ring substituents enhance the compound's binding affinity to target enzymes, thereby increasing herbicidal efficacy at lower application rates.
Solution Approach 2:
The patent creates composite molecular structures by combining the phenyltriazolinone core with various aromatic substituents (pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl rings) and diverse functional groups. These composite structures leverage synergistic electronic and steric effects to improve herbicidal activity, allowing effective control of harmful plants at reduced application rates while maintaining crop safety.
2Reliability
If existing phenyltriazolinone herbicides are used, then herbicidal action is achieved, but compatibility with crop plants is insufficient
Solution Approach 1:
The patent applies local quality by introducing specific substituents at particular positions of the phenyltriazolinone molecule that enhance selectivity. For example, substitutions at R1-R3 positions with alkyl, haloalkyl, or hydrogen groups, combined with specific R4-R6 substitutions, create a molecular configuration that preferentially binds to weed target sites while having reduced affinity for crop plant enzymes, thereby improving crop compatibility.
Solution Approach 2:
The patent uses the modified phenyltriazolinone compounds as selective intermediaries that exploit metabolic or structural differences between crop plants and harmful plants. The specific substituent patterns act as molecular mediators that allow the herbicide to be activated or bind effectively only in harmful plants, sparing crop plants from damage while maintaining herbicidal efficacy.
3Reliability
If herbicidal activity is enhanced through structural modifications, then control of harmful plants improves, but structural complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the phenyltriazolinone molecule into distinct functional segments: the core triazolinone ring (positions Q, W, X, Y), the aromatic substituent Z with vicinal carbon atom attachment, and variable R1-R7 groups. This segmented approach allows independent optimization of each segment's contribution to herbicidal activity, managing molecular complexity while enhancing efficacy through systematic substitution patterns.
Data Source
AI summary
The present invention relates to phenyltriazolinones of formula (I)or their agriculturally acceptable salts or derivatives, wherein the variables are defined according to the description, processes and intermediates for preparing the uracilpyryidines of the formula (I), compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one urycilpyridine of the formula (I) to act on plants, their seed and/or their habitat.


