A series of methyl 6-Chloro-2-Substitued-1-[2-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]1H-benzoimidazol-5-ylamine were successfully synthesized. Benzimidazoles were prepared by condensation of 4-chloro-o-phenylenediamine with substituted aryl, aldehyde condensation with biphenyl tetrazole group and reduction stannous chloride dihydrate. An insertion-cyclization strategy was involved during synthe...

α,β-Unsaturated acyl ammoniums generated from the reaction of α,β-unsaturated 2,4,6-trichlorophenol (TCP) esters bearing a pendent enone with an isothiourea organocatalyst are versatile intermediates in a range of enantioselective nucleophile-dependent domino processes to form complex products of diverse topology with excellent stereoselectivity. Use of either 1,3-dicarbonyls, acyl benzothiazol...

A general and efficient phosphorous acid-catalyzed cyclocondensation of β-ketoesters with o-aminobenzamides via selective C-C bond cleavage leading to quinazolinones is developed. This reaction proceeds smoothly under metal- and oxidant-free conditions, giving both 2-alkyl- and 2-aryl-substituted quinazolinones in excellent yields. This strategy can also be applied to the synthesis of other N-h...

1-Methyl-3-(2-oxyethyl)-1H-Imidazol-3-ium-Borate Sulfonic Acid ([MOEI]-BSA) was easily prepared and used as a new and highly efficient solid acid catalyst for the synthesis of benzimidazole derivatives with high isolated yields. Various substituted benzimidazoles were synthesized by a combination of o-phenylenediamines and aldehydes in the presence of [MOEI]-BSA with excellent yields in water a...

Diversity-oriented synthesis of novel benzimidazole linked indolo-benzodiazepine/quinoxaline ring systems using poly(ethylene glycol) as soluble polymer support is described. Commercially available 4-fluoro-3-nitrobenzoic acid and indoline were utilized for the construction of these annulated biheterocyclic compound libraries having multiple privileged structures with three-point structural div...

1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU) is a novel and active catalyst in promoting the methylation reaction of phenols, indoles, and benzimidazoles with dimethyl carbonate under mild conditions. Additional rate enhancement is accomplished by applying microwave irradiation. By incorporating tetrabutylammonium iodide, the same microwave reactions can be further accelerated. By combining these a...

Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia...