40853-32-5Relevant academic research and scientific papers
Methanol as the C1source: Redox coupling of nitrobenzenes and alcohols for the synthesis of benzimidazoles
An, Jie,Lai, Zemin,Li, Hengzhao,Peng, Mengqi,Sun, Yanhao,Yan, Zihan,Yang, Ruoyan,Zhang, Yuntong
supporting information, p. 748 - 753 (2022/02/02)
We present an operationally simple redox coupling for the synthesis of N-1 substituted benzimidazoles using feedstock building block 2-nitroaniline derivatives as the precursors and methanol as the C1 source. Higher atom, step, and redox economies and exc
Convenient synthesis of N-1-alkyl benzimidazoles via Pd catalyzed C–N bond formation and cyclization
Bie, Fusheng,Yao, Yongfeng,Cao, Han,Shi, Yijun,Yan, Peng,Ma, Jie,Han, Ying,Liu, Xuejing
, p. 2387 - 2396 (2021/06/25)
N-1-Alkyl-2-unsubstituted benzimidazoles were directly synthesized by intermolecular coupling of formimidamides with benzylamines; the syntheses were catalyzed by Pd(OAc)2 in one pot, giving rise to moderate to good yields. Aromatic formamidine
High-Throughput Screening of Reductive Amination Reactions Using Desorption Electrospray Ionization Mass Spectrometry
Cooks, R. Graham,Ferreira, Christina R.,Li, Yangjie,Logsdon, David L.,Paschoal Sobreira, Tiago Jose,Thompson, David H.
supporting information, p. 1647 - 1657 (2020/10/26)
This study describes the latest generation of a high-throughput screening system that is capable of screening thousands of organic reactions in a single day. This system combines a liquid handling robot with desorption electrospray ionization (DESI) mass spectrometry (MS) for a rapid reaction mixture preparation, accelerated synthesis, and automated MS analysis. A total of 3840 unique reductive amination reactions were screened to demonstrate the throughputs that are capable with the system. Products, byproducts, and intermediates were all monitored in full-scan mass spectra, generating a complete view of the reaction progress. Tandem mass spectrometry experiments were conducted to verify the identity of the products formed. The amine and electrophile reactivity trends represented in the data match what is expected from theory, indicating that the system accurately models the reaction performance. The DESI results correlated well with those generated using more traditional mass spectrometry techniques like liquid chromatography-mass spectrometry, validating the data generated by the system.
Synthesis method of benzimidazole compound based on iron catalytic oxidation-reduction coupling reaction
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Paragraph 0094-0098, (2020/10/05)
The invention belongs to the field of organic synthesis, and relates to a benzimidazole compound synthesis method based on an iron catalytic oxidation-reduction coupling reaction. According to the method, o-nitroaniline compounds and alcohol compounds are used as raw materials, and the benzimidazole compounds are generated through iron-catalyzed redox coupling reaction in the presence of an iron catalyst and a proton donor. The method provided by the invention provides a new way for the synthesis of benzimidazole drugs and pesticides. Compared with a traditional benzimidazole compound synthesis method with o-phenylenediamine compounds and carboxylic acid or carboxylic acid derivatives as raw materials, the method has the advantages that the atom utilization rate of the whole process is increased, the production cost is reduced, and waste gas, waste liquid and waste solid generated in the production process is reduced.
Method for synthesizing metal-catalyzed 1-benzylamino substituted benzimidazole
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Paragraph 0055-0057, (2019/01/08)
The invention provides a method for synthesizing metal-catalyzed 1-benzylamino substituted benzimidazole, and the metal-catalyzed 1-benzylamino substituted benzimidazole is prepared from raw materialso-halogenated aryl N, N-dimethylformamidine or a deriva
TNF -Alpha Modulating Benzimidazoles
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Paragraph 0494, (2015/06/10)
A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Facile one-pot synthesis of N-alkylated benzimidazole and benzotriazole from carbonyl compounds
Meng, Xu,Li, Xiaolong,Chen, Wenlin,Zhang, Yuanqing,Wang, Wen,Chen, Jinying,Song, Jinli,Feng, Huijie,Chen, Baohua
, p. 349 - 356 (2014/04/17)
An efficient one-pot N-alkylation of benzimidazole and benzotriazole from carbonyl compounds and tosylhydrazide has been accomplished via copper powder-catalyzed N - H bond insertion affording N-alkylated products in good yields. The reaction can tolerate a wide range of carbonyl compounds, such as aryl, alkyl, heterocyclic and α,β-unsaturated ketones, and aldehydes.
Direct C-N coupling of imidazoles and benzylic compounds via iron-catalyzed oxidative activation of C-H bonds
Xia, Qinqin,Chen, Wanzhi,Qiu, Huayu
experimental part, p. 7577 - 7582 (2011/11/12)
Iron-catalyzed direct C-N bond formation between imidazoles and benzylic hydrocarbons is described. The reaction utilizes an inexpensive iron catalyst-oxidant system that is suitable for the coupling of a range of benzylic C-H bonds with various imidazoles.
