16931-35-4Relevant academic research and scientific papers
BICYCLIC HETEROARYL DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
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Paragraph 0373, (2020/10/21)
The present disclosure provides certain bicyclic heteroaryl compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I). Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Transition-metal and oxidant-free approach for the synthesis of diverse N-heterocycles by TMSCl activation of isocyanides
Chen, Fen-Er,Dong, Lin,Li, Hongyan,Liu, Jinxin,Luo, Liangliang,Xiao, You-Cai,Zhou, Yuan
, p. 29257 - 29262 (2020/10/02)
A highly efficient TMSCl-mediated addition of N-nucleophiles to isocyanides has been achieved. This transition-metal and oxidant-free strategy has been applied to the construction of various N-heterocyles such as quinazolinone, benzimidazole and benzothiazole derivatives by the use of distinct amino-based binucleophiles. The notable feature of this protocol includes its mild reaction condition, broad functional group tolerance and excellent yield. This journal is
Microwave use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds method
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Paragraph 0071, (2019/03/28)
The invention discloses a microwave the use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds, in the aqueous phase under microwave conditions adding benzoic amidine compound under alkaline condition [...] into benzimidazole reaction, invention an environment-friendly, the operation is simple, cheap and safe, efficient process for preparing benzimidazole method. Compared with the prior art, this method not only can be applied to a large number of functional groups, the productive rate is high, few by-products, and the operation is simple, safe, low cost, environmental protection; .
Benzimidazole CB2 agonists: Design, synthesis and SAR
Nanda, Kausik K.,Henze, Darrell A.,Della Penna, Kimberly,Desai, Reshma,Leitl, Michael,Lemaire, Wei,White, Rebecca B.,Yeh, Suzie,Brouillette, Janine N.,Hartman, George D.,Bilodeau, Mark T.,Trotter, B. Wesley
, p. 1218 - 1221 (2014/03/21)
A new series of CB2-selective agonists containing a benzimidazole core is reported. Design, synthesis, SAR and pharmacokinetic data for selected compounds are described.
Ultrasound promoted expeditious, catalyst-free and solvent-free approach for the synthesis of N,N′-diarylsubstituted formamidines at room temperature
Dar, Bashir Ahmad,Ahmad, Syed Naseer,Wagay, Mohammad Arif,Hussain, Altaf,Ahmad, Nisar,Bhat, Khursheed Ahmad,Khuroo, Mohammad Akbar,Sharma, Meena,Singh, Baldev
, p. 4880 - 4884 (2013/09/02)
An effortless and efficient protocol was developed for the synthesis of N,N′-diarylsubstituted formamidines under environment-friendly conditions. Ultrasonic energy was employed to obtain the desired products in excellent yields with high purity under solvent-free and catalyst-free conditions. Products were purified by the crystallization technique to avoid excess utilization of organic solvents.
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation
De La Fuente, Tania,Martín-Fontecha, Mar,Sallander, Jessica,Benhamú, Bellinda,Campillo, Mercedes,Medina, Rocío A.,Pellissier, Lucie P.,Claeysen, Sylvie,Dumuis, Aline,Pardo, Leonardo,López-Rodríguez, María L.
experimental part, p. 1357 - 1369 (2010/08/20)
On the basis of our previously described pharmacophore model for serotonin 5-HT6 receptor (5-HT6R) antagonists, we have designed, synthesized, and pharmacologically characterized a series of benzimidazole derivatives 1-20 that repres
Mild and general one-pot reduction and cyclization of aromatic and heteroaromatic 2-nitroamines to bicyclic 2 H -imidazoles
Hanan, Emily J.,Chan, Bryan K.,Estrada, Anthony A.,Shore, Daniel G.,Lyssikatos, Joseph P.
experimental part, p. 2759 - 2764 (2010/12/25)
A one-pot procedure for the conversion of aromatic and heteroaromatic 2-nitroamines into bicyclic 2H-benzimidazoles is described. The procedure employs formic acid, iron powder, and an additive such as NH4Cl to reduce the nitro group and effect the imidazole cyclization with high-yielding conversions generally within one to two hours. The compatibility with a wide range of functionality demonstrates the general utility of this procedure.
