Diaryl-Azole Compounds for Pest Control
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Solution Overview
Problem
Current agrochemicals face challenges in providing effective insecticidal and acaricidal activity while ensuring safety for plants, livestock, and humans, and are often rendered ineffective by resistant pest strains.
Innovation Solution
Development of diaryl-azole compounds with specific structural formulas that exhibit superior insecticidal and acaricidal activity, are industrially synthesizable, and have reduced toxicity and phytotoxicity, including formulations for controlling ectoparasites and endoparasites.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional agrochemicals are used to control harmful organisms, then insecticidal and acaricidal activity is achieved, but chemical resistance develops and toxicity to plants and animals increases
Solution Approach 1:
The patent modifies the chemical structure of diaryl-azole compounds by changing parameters such as substituting hydrogen atoms with halogen atoms (fluoro, chloro, bromo, iodo) at specific positions (R2, R3, R6), and introducing various functional groups (cyano, nitro, carbonyl, carboxyl, ester, amide, urea, carbamate, isocyanate, isocyanato, isocarbamate, hydroxyl, alkoxy, aryloxy, etc.). These structural parameter changes result in compounds with superior insecticidal and acaricidal activity while reducing toxicity to plants and animals compared to conventional agrochemicals.
2Reliability
If existing diaryl-azole compounds are synthesized, then insecticidal activity is obtained, but the synthesis process is complex and costly
Solution Approach 1:
The patent divides the diaryl-azole compound into distinct structural segments: a core diaryl-azole skeleton with independently variable substituents at different positions (R1-R6). This segmentation allows for modular synthesis where each substituent can be introduced or modified independently, simplifying the overall synthesis process and reducing costs while maintaining superior insecticidal activity.
3Reliability
If higher concentrations of agrochemicals are used to control resistant pest strains, then efficacy is improved, but phytotoxicity and environmental contamination increase
Solution Approach 1:
The patent creates composite molecular structures by combining the diaryl-azole core with various functional groups and substituents (halogen atoms, cyano groups, carbonyl groups, carboxyl groups, ester groups, amide groups, urea groups, carbamate groups, isocyanate groups, isocyanato groups, isocarbamate groups, hydroxyl groups, alkoxy groups, aryloxy groups, etc.). These composite structures enable the compound to achieve high efficacy against resistant pest strains at lower concentrations, thereby reducing phytotoxicity and soil contamination.
Data Source
AI summary
A compound represented by Formula (I), or a salt thereof:wherein, R1 represents an unsubstituted or substituted C1-6 alkylthio group, or the like; A1 represents a nitrogen atom or CH; A2 represents a nitrogen atom or CR2; R2 and R3 each independently represents a hydrogen atom, an unsubstituted or substituted C6-10 aryl group, an unsubstituted or substituted 3- to 6-membered heterocyclyl group, or the like; B1 and B2 each independently represents a nitrogen atom or CR5, with the proviso that B1 and B2 do not represent CR5 at the same time, wherein R5 represents a hydrogen atom, an unsubstituted or substituted C1-6 alkyl group, or the like; R4 represents an unsubstituted or substituted C1-6 alkyl group, or the like, and R4 binds to any one of nitrogen atoms forming an imidazole ring or a triazole ring; and Ar represents an unsubstituted or substituted C6-10 aryl group or the like.