500011-86-9Relevant articles and documents
Design, synthesis and insecticidal-activity evaluation of N-pyridylpyrazolo-5-methyl amines and its derivatives
Yang, Shuai,Xu, Kaijie,Lai, Qiuqin,Zhao, Chen,Xu, Hanhong
, p. 4304 - 4311 (2020)
In searching for novel insecticidal leads, a series of N-pyridylpyrazolo-5-methyl amines and their derivatives were designed and synthesized. Among the 22 target compounds obtained, bioassays indicated that some of the target compounds exhibited good insecticidal activities against Plutella xylostella (P. xylostella) and Spodoptera frugiperda (S. frugiperda). In particular, compound 9j revealed the best insecticidal activity against P. xylostella, with a LC50 value of 22.11 mg/L, and compound 9q had the best insecticidal activity against S. frugiperda which with 73.99% of mortality rate at 100 mg/L. Structure-activity relationship (SAR) analysis showed that 4-CF3 at the position of R1 linked with N-pyridylpyrazole via amide bond could enhance the insecticidal activity of the target compounds. This study provides valuable clues for the further design and optimization of N-pyridylpyrazole derivatives.
Method for synthesizing chlorantraniliprole
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Paragraph 0024; 0029; 0032; 0037; 0040; 0045, (2021/10/11)
A solvent containing 2 - amino -3 - methylbenzoic acid is stirred, N - methyl -3 - methyl -2 - amino - benzamide is dissolved in alkali liquor in a stirring reaction process, and reacted with NCS to obtain N - methyl -3 - methyl -2 - amino -5 - chloro - benzamide. The reaction of the bromination reaction, the oxidation reaction and the condensation reaction is carried out by cooperation of a catalyst so as to obtain chlorantraniliprole. By optimizing the preparation steps of chlorantraniliprole, the whole process is relatively simple in process steps, the post-treatment is simple, intermediate products can be obtained directly after the single step is finished, high environmental control requirements are not needed in the whole synthesis step, and industrialization can be conveniently realized.
Preparation method of key intermediate K acid of chlorantraniliprole
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Paragraph 0004; 0011, (2021/02/06)
The invention relates to a preparation method of a key intermediate K acid of chlorantraniliprole. The preparation method has the advantages of fewer reaction sites, less impurity generation and capability of realizing efficient, green and environment-friendly preparation of K acid. According to the method, ethyl acetoacrylate is used as a raw material and subjected to carbonyl protection, cyclization, deprotection, oxidation and bromination so as to finally prepare the K acid. The method has the advantages of high cyclization yield, good selectivity and high product purity.