1093966-37-0Relevant articles and documents
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
Yang, Bowen,Wu, Qian,Huan, Xiajuan,Wang, Yingqing,Sun, Yin,Yang, Yueyue,Liu, Tongchao,Wang, Xin,Chen, Lin,Xiong, Bing,Zhao, Dongmei,Miao, Zehong,Chen, Danqi
supporting information, (2020/12/28)
In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target.
Arylpyrazol ester compound and synthesis method and application thereof
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Paragraph 0033; 0037-0038; 0044; 0048-0049; 0054; 0058-0059, (2019/10/07)
The invention relates to an arylpyrazol ester compound and a synthesis method and application thereof. The compound is applied to a pesticide intermediate. The synthesis method of the compound comprises the following steps: 1)taking 2-amino-3-methyl benzonitrile as a raw material, and reacting with bromide to obtain 2-amino-5-bromo-3-methyl benzonitrile; 2) dehydrogenizing the 2-amino-5-bromo-3-methyl benzonitrile to obtain 2,2'-(diazene-1,2-diyl)bis(5-bromo-3-methyl benzonitrile); 3) performing a reaction on the 2,2'-(diazene-1,2-diyl)bis(5-bromo-3-methyl benzonitrile) with ethyl alcohol to obtain the compound. Compared with the prior art, according to the arylpyrazol ester compound and the synthesis method and application thereof, the arylpyrazol ester compound 5-bromo-2-(5-bromo-7-methyl-3-ethoxycarbonyl-2H-indazole-2-yl)-3-methyl benzonitrile is synthesized by taking the 2-amino-3-methyl benzonitrile as the raw material through three steps of reaction; the synthetic process of the compound is simple; the operation steps are simplified; the generation of three wastes (waste gas, waste water and industrial residue) substances is reduced; relatively high product purity is realized.