4-Pyridinyl Formamide Herbicides for Resistant Weed Control

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Solution Overview

Problem

The increasing resistance of weeds to existing herbicides, particularly ALS inhibitors and ACCe inhibitors, necessitates the development of new herbicides with higher efficiency, safety, and selectivity for crops like wheat and rice, while addressing environmental concerns.

Innovation Solution

A 4-pyridinyl formamide compound or derivative thereof, characterized by specific substituents, exhibits excellent herbicidal activity and crop safety, offering selectivity for key crops such as wheat and rice.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing herbicides (ALS inhibitors and ACCe inhibitors) are used for weed control, then weed control effect is achieved, but weed resistance increases

Engineering Contradiction:
Improveweed control effectVSAvoidweed resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical structure parameters by introducing a 4-pyridinyl formamide core structure with specific substituents (X, Y, M, R1-R6 groups), creating a new herbicide class that differs fundamentally from existing ALS and ACCe inhibitors. This structural parameter change enables the compound to overcome weed resistance while maintaining herbicidal activity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite molecular structure combining a pyridinyl ring system with formamide linkage and various substituent groups (halogen, cyano, nitro, alkyl, aryl, heteroaryl groups). This composite structure integrates multiple functional groups that work synergistically to achieve both weed control and crop safety, addressing the resistance problem through structural complexity

Inventive Principle:
Principle #40Composite materials

2Reliability

If new herbicides are developed to overcome resistance, then herbicidal activity is improved, but crop safety may be compromised

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

Solution Approach 1:

The patent applies local quality by introducing specific substituent groups at defined positions on the pyridinyl formamide core structure. Different substituents (electron-withdrawing groups like halogen, cyano, nitro at X and Y positions; various alkyl, aryl, heteroaryl groups at M and R1-R6 positions) create localized electronic and steric effects that enhance herbicidal activity while maintaining selectivity for crop safety

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent creates a dynamic series of derivatives by varying substituents at multiple positions (X, Y, M, R1-R6) on the core structure. This allows optimization of the balance between herbicidal activity and crop safety through systematic structural modification, enabling selection of compounds with desired activity-safety profiles

Inventive Principle:
Principle #15Dynamics

3Reliability

If herbicide effectiveness is maintained against resistant weeds, then weed control is achieved, but environmental impact increases

Engineering Contradiction:
Improveweed control effectivenessVSAvoidenvironmental impact
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes chemical parameters by developing a new molecular class with improved metabolic stability and reduced non-target effects. The pyridinyl formamide structure with specific substituents provides enhanced selectivity and reduced environmental persistence compared to conventional herbicides, maintaining effectiveness while reducing harm

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12497365B24-pyridinyl formamide compound or derivative thereof, preparation method therefor, herbicidal composition and use thereof
Publication Date: 2025.12.16 QINGDAO KINGAGROOT CHEM COMPOUNDS CO LTD

AI summary

The invention belongs to the technical field of pesticides, and specifically relates to a 4-pyridinyl formamide compound or a derivative thereof, a preparation method therefor, a herbicidal composition and the use thereof. The 4-pyridinyl formamide compound is as represented by formula (I), wherein, X and Y each independently represent nitro, halogen, cyano, formyl, thiocyano, mercapto, etc.; and M represents an unsubstituted or substituted structure (II). The compound, and the derivative and the composition thereof have excellent herbicidal activity and a higher crop safety, and establish good selectivity, especially for key crops such as wheat and rice.