73457-35-9Relevant academic research and scientific papers
Nickel-Catalyzed C-O Cross-Coupling Reaction at Low Catalytic Loading with Weak Base Participation
Wu, Fan,Zhu, Kejie,Wu, Guolin,Gao, Yu,Chen, Haijun
supporting information, p. 519 - 522 (2020/01/30)
Herein, we report a nickel-catalyzed crossing-coupling reaction for the synthesis of diaryl ethers. The desired products are achieved by coupling heterocyclic alcohols with aryl bromides bearing strong electron withdrawing nitro group under the catalyst system of NiCl2(PPh3)2 and weak base KHCO3. This mild reaction exhibits a broad functional group tolerance. Compound 4 as an important intermediate is suitable for further structural modification of MALT1 inhibitor MI-2.
Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors
Wu, Guolin,Wang, Haixia,Zhou, Wenhui,Zeng, Bihua,Mo, Wenhui,Zhu, Kejie,Liu, Rong,Zhou, Jia,Chen, Ceshi,Chen, Haijun
supporting information, p. 3321 - 3344 (2018/05/23)
Recent studies revealed that MALT1 is a promising therapeutic target for the treatment of ABC-DLBCL. Among several reported MALT1 inhibitors, MI-2 as an irreversible inhibitor represents a new class of ABC-DLBCL therapeutics. Due to its inherent potential cross-reactivity, further structure–activity relationship (SAR) study is imperative. In this work, five focused compound libraries based on the chemical structure of MI-2 are designed and synthesized. The systematic SARs revealed that the side chain of 2-methoxyethoxy has little impact on the activity and can be replaced by other functionalized groups, providing new MI-2 analogues with retained or enhanced potency. Compounds 81–83 with terminal hydroxyl group as side chain displayed enhanced activities against MALT1. Replacement of triazole core with pyrazole is also tolerant, while structural modifications on other sites are detrimental. These findings will facilitate further development of small-molecule MALT1 inhibitors.
1,3,5-trisubstituted pyrazole compound as well as preparation method and application thereof
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Paragraph 0019; 0020; 0021; 0022; 0023; 0024; 0025, (2017/10/07)
The invention discloses a 1,3,5-trisubstituted pyrazole compound as well as a preparation method and application thereof. The 1,3,5-trisubstituted pyrazole compound is 5-(3,4-dichlorophenyl)-3-(4-(2-chloroacetylamino) phenoxyl)-1-(2-methoxyethyl)pyrazole,
