Pyrazolone Herbicide Selectivity via Local Quality

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Solution Overview

Problem

Current herbicides are inefficient in controlling a broad spectrum of weeds, particularly perennial species, and often damage crops, necessitating the development of more effective and selective herbicides with reduced impact on economically important crops.

Innovation Solution

A novel pyrazolone compound and its salt, characterized by specific structural substitutions, are synthesized for use in herbicidal compositions, offering broad-spectrum herbicidal activity with minimal impact on desirable crops, including genetically modified plants, and can be applied pre-sowing, pre-emergence, or post-emergence.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing herbicides are used to control weeds, then herbicidal activity is achieved, but crop damage occurs and efficacy against perennial weeds is insufficient

Engineering Contradiction:
Improveherbicidal activityVSAvoidcrop damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by introducing specific substituent groups (R1, R2, R3, R4, R5, R6) at different positions of the pyrazolone core structure. Each position can be independently substituted with specific functional groups (halogens, alkyls, alkoxy, carboxy, etc.) to optimize the balance between herbicidal activity and crop safety. This localized modification of molecular structure allows differential action on weeds versus crops.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying multiple structural parameters of the pyrazolone compound including: the type of nitrogen-containing heterocyclic group, the substitution patterns at positions 1-6, the nature of substituent groups (fluorine, chlorine, methyl, ethyl, methoxyl, etc.), and the presence/absence of carbonyl groups. These parameter variations enable fine-tuning of herbicidal selectivity and efficacy.

Inventive Principle:
Principle #35Parameter changes

2Use of energy by moving object

If hand or mechanical weeding is used, then labor and energy consumption are reduced, but weed control effectiveness is insufficient

Engineering Contradiction:
Improvelabor and energy consumptionVSAvoidweed control effectiveness
Core Design Contradiction:
Use of energy by moving objectVSReliability

Solution Approach 1:

The patent replaces mechanical weeding systems with chemically-based pyrazolone herbicides that provide superior weed control effectiveness. The chemical compounds act systematically on weed physiological processes, achieving complete control that mechanical methods cannot provide, while requiring minimal application effort compared to repeated mechanical weeding operations.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Reliability

If chemical weed control methods are applied, then weed control effectiveness is improved, but the complexity of herbicide structures increases

Engineering Contradiction:
Improveweed control effectivenessVSAvoidherbicide structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent achieves universality by designing a pyrazolone core structure (formula I) that can control multiple types of weeds (monocotyledonous and dicotyledonous, annual and perennial) through systematic substitution at six different positions. This single molecular framework with variable substituents provides broad-spectrum herbicidal activity, eliminating the need for multiple different herbicide molecules.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS11076594B2Pyrazolone compound or salt thereof, preparation method therefor, herbicide composition and use thereof
Publication Date: 2021.08.03 QINGDAO KINGAGROOT CHEM COMPOUNDS CO LTD
  • US11076594B2 patent drawing
  • US11076594B2 patent drawing
  • US11076594B2 patent drawing

AI summary

The present invention belongs to the field of pesticides, particularly relates to a pyrazolone compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. The pyrazolone compound is as described in formula I:In the formula, R1R2N represents substituted or unsubstituted 3-8 membered nitrogen-containing heterocyclic group containing 1-3 heteroatoms; or R1 and R2 each represent hydrogen or C1-8 alkyl; R3 represents hydrogen, C1-4 alkyl, alkenyl, alkynyl, unsubstituted C3-6 cycloalkyl or C3-6 cycloalkyl substituted by C1-4 alkyl; R4 represents methyl, ethyl, n-propyl, isopropyl or cyclopropyl; X represents hydrogen, —S(O)nR6, —R7 or substituted or unsubstituted 3-8 membered heterocyclic group containing 1-4 heteroatoms, wherein, n represents 1, 2 or 3, R6 represents substituted or unsubstituted alkyl or aryl, and R7 represents substituted or unsubstituted alkyl, aryl, alkyl acyl or aroyl. The active substance of the invention exhibits good herbicidal effect, and is convenient to use, low in cost and has great commercial value.