23982-86-7Relevant articles and documents
Benzimidazole compound with endothelial lipase inhibition effect and application of benzimidazole compound
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Paragraph 0097; 0130-0132; 0137, (2020/12/09)
The invention discloses a benzimidazole compound with an endothelial lipase inhibition effect and application of the benzimidazole compound, and belongs to the technical field of medicines. The benzimidazole compound has an excellent inhibition effect on endothelial lipase, can effectively treating atherosclerosis and sequelae thereof, such as coronary heart disease, and also promotes treatment onmetabolic syndrome and sequelae thereof, such as diabetes. The benzimidazole compound provided by the invention has good solubility in an aqueous medium, also has good biological activity and metabolic stability, and shows advantages in the aspect of serum stability.
One-pot strategy of copper-catalyzed synthesis of 1,2-disubstituted benzimidazoles
Xie, Caixia,Han, Xushuang,Gong, Jian,Li, Danyang,Ma, Chen
, p. 5811 - 5819 (2017/07/22)
A simple, one-pot and copper-catalyzed coupling reaction for the construction of 1,2-disubstituted benzimidazole derivatives is described. A low-cost copper salt and a weak base K3PO4 were utilized in this reaction. A variety of 1,2-disubstituted benzimidazoles were obtained in moderate to excellent yields.
"All-water" one-pot diverse synthesis of 1,2-disubstituted benzimidazoles: Hydrogen bond driven 'synergistic electrophile-nucleophile dual activation' by water
Kommi, Damodara N.,Jadhavar, Pradeep S.,Kumar, Dinesh,Chakraborti, Asit K.
, p. 798 - 810 (2013/04/24)
A new "all-water" tandem arylaminoarylation/arylaminoalkylation- reduction-cyclisation route is reported for one-pot diversity oriented synthesis of regiodefined 1,2-disubstituted benzimidazoles. Water plays a crucial and indispensable role through hydrogen bond driven 'synergistic electrophile-nucleophile dual activation' in the formation of N-mono-aryl/aryl alkyl/alkyl/cycloalkyl o-nitroanilines under metal and base-free conditions to replace the transition metal-based C-N bond formation (aryl amination) chemistry and underlines the origin of regiodefined installation of the diverse selection of aryl, aryl alkyl, and alkyl/cycloalkyl groups as substituents on the benzimidazole scaffold to form the 1,2-disubstituted benzimidazoles. The influence of the hydrogen bond effect of water in promoting the arylaminoarylation reaction under base and metal-free conditions has been realized through observation of inferior yields in D2O compared to that obtained in water during the reaction of o-fluoronitrobenzene with aniline separately performed in water and D2O under similar experimental conditions. Water also provides assistance in promoting the subsequent nitro reduction and in the final cyclocondensation steps. The role of water in promoting the cyclocondensation reaction through hydrogen bonds is realized by the differential product yields during the reaction of mono-N-phenyl-o- phenylenediamine with benzaldehyde performed separately in water and D 2O. The better hydrogen bond donor and hydrogen bond acceptor abilities of water compared to those of the organic solvents are the contributing/deciding factors for making the new water-assisted tandem arylaminoarylation/arylaminoalkylation-reduction-cyclisation strategy for the diversified synthesis of the regiodefined 1,2-disubstituted benzimidazoles effective in an aqueous medium, making it represent a true "all-water chemistry."
