Malonamide Herbicides: Enhancing Selectivity and Reducing Toxicity
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Solution Overview
Problem
Current malonamide compounds for controlling unwanted vegetation lack sufficient herbicidal activity, selectivity, and compatibility with crop plants, often resulting in higher toxicity to humans and animals.
Innovation Solution
Development of malonamide compounds of formula (I) with specific substituents that enhance herbicidal activity, selectivity, and compatibility, including their agriculturally acceptable salts, amides, esters, or thioesters, for use as herbicides to control unwanted vegetation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional malonamide compounds are used for controlling unwanted vegetation, then herbicidal activity is achieved, but the activity is insufficient at low application rates and selectivity is unsatisfactory
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns at defined positions (R1-R8) of the malonamide core structure. Different substituents are placed at specific locations to create localized functional regions that enhance both herbicidal activity through improved target binding and selectivity through differential uptake or metabolism by unwanted versus crop plants.
Solution Approach 2:
The patent employs parameter changes by systematically varying substituent types, sizes, and positions on the malonamide scaffold. This includes modifying electronic properties through different functional groups and steric properties through varying chain lengths and cyclic structures, thereby optimizing the balance between herbicidal potency and crop safety.
2Reliability
If conventional malonamide compounds are used, then herbicidal effect is achieved, but toxicity to humans and animals is high
Solution Approach 1:
The patent uses local quality by incorporating specific substituent configurations that enhance herbicidal mechanism specificity. The modified structures are designed to interact preferentially with plant-specific targets while minimizing interaction with mammalian biological systems, thereby reducing toxicity to humans and animals.
Solution Approach 2:
The patent applies this principle by designing compounds where the structural modifications that reduce mammalian toxicity do not compromise herbicidal efficacy. The altered malonamide structures exploit differences in metabolic pathways between plants and animals, converting potential harm to non-target organisms into a beneficial selectivity advantage.
3Reliability
If conventional malonamide compounds are used, then herbicidal activity is achieved, but compatibility with crop plants is low
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns that create differential interactions with crop versus unwanted plants. The modified malonamide structures are designed to be selectively taken up or metabolized by unwanted plants while remaining compatible with crop plants through avoided interaction with crop-specific targets or metabolic pathways.
Solution Approach 2:
The patent uses inversion by reversing the traditional approach: instead of designing compounds that actively harm crop plants and then trying to reduce that harm, the invention designs compounds from the outset to specifically avoid interacting with crop plant targets, inverting the selectivity design philosophy to achieve inherent crop safety.
Data Source
AI summary
The invention relates to compounds of formula (I), and their use as herbicides. In said formula, R1 to R8 represent groups such as hydrogen, halogen or organic groups such as alkyl, alkenyl, alkynyl, or alkoxy; X is a bond or a divalent unit; Y is hydrogen, cyano, hydroxyl or a linear or cyclic organic group. The invention further refers to a composition comprising such compound and to the use thereof for controlling unwanted vegetation.