3968-04-5

Upstream product

• 161468-86-6 2-Oxo-3-(toluene-4-sulfonyl)-2,3-dihydro-benzoimidazole-1-carboxylic acid ethyl ester 
• 615-16-7 1,3-dihydro-2H-benzimidazol-2-one 
• 41120-23-4 ethyl 2-oxo-2,3-dihydro-1H-benzo[d]imidazole-1-carboxylate 
• 400090-87-1 N-hydroxy-2-(4-methylphenylsulfonamido)benzamide 
• 95-54-5 1,2-diamino-benzene 
• 161468-45-7 tert‐butyl 2‐oxo‐2,3‐dihydro‐1H‐benzo[d]imidazole‐1‐carboxylate 
• 361535-25-3 2,3-dihydro-2-oxo-3-(4-tolylsulfonyl)-1H-benzimidazole-1-carboxylic acid 1,1-dimethylethyl ester 

Relevant academic research and scientific papers

N-arylsulfonyl-benzimidazolones as potential hypoglycemic agents

1,3-Bis(arylsulfonyl)-benzimidazolones 1a-d were synthesized by reacting benzimidazolones with arenesulfonyl chlorides in the presence of NaOH. Mono(arylsulfonyl)-benzimidazolone derivatives 5a-c were prepared from benzimidazolone by protecting one of the

P(III)-Assisted Electrochemical Access to Ureas via in situ Generation of Isocyanates from Hydroxamic Acids

An external oxidant-free protocol for the generation of isocyanates from hydroxamic acids assisted by trivalent phosphine under mild electrochemical conditions was reported. The process started with the anodic oxidation of hydroxamic acids, followed by reacting with phosphine to form corresponding alkoxyphosphoniums and subsequent rearrangement with the release of tri-substituted phosphine oxide as the driving force to give isocyanates, which were trapped by N-based nucleophiles to produce various ureas. This method provides a broadly applicable procedure to access isocyanate intermediates under mild electrochemical conditions.

Conjugates of degraded and oxidized hydroxyethyl starch and sulfonylureas: Synthesis, characterization, and in vivo antidiabetic activity

Orally administered drugs usually face the problem of low water solubility, low permeability, and less retention in bloodstream leading to unsatisfactory pharmacokinetic pro file of drugs. Polymer conjugation has attracted increasing interest in the pharmaceutical industry for delivering such low molecular weight (Mw) drugs as well as some complex compounds. In the present work, degraded and oxidized hydroxyethyl starch (HES), a highly biocompatible semisynthetic biopolymer, was used as a drug carrier to overcome the solubility and permeability problems. The HES was coupled with synthesized N-arylsulfonylbenzimidazolones, a class of sulfonylurea derivatives, by creating an amide linkage between the two species. The coupled products were characterized using GPC, FT-IR, 1H NMR, and 13C NMR spectroscopy. The experiments established the viability of covalent coupling between the biopolymer and N-arylsulfonylbenzimidazolones. The coupled products were screened for their in vivo antidiabetic potential on male albino rats. The coupling of sulfonylurea derivatives with HES resulted in a marked increase of the hypoglycemic activity of all the compounds. 2,3-Dihydro-3-(4-nitrobenzensulfonyl)-2-oxo-1H-benzimidazole coupled to HES10100 was found most potent with a 67% reduction in blood glucose level of the rats as compared to 41% reduction produced by tolbutamide and 38% by metformin. (Chemical Equation Presented).

Regiospecific functionalization of 1,3-dihydro-2H-benzimidazol-2-one and structurally related cyclic urea derivatives

Methods for selectively protecting one of the degenerate nitrogen atoms of the cyclic urea derivatives 1,3-dihydro-2H-benzimidazol-2-one (6a), 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (11), 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones (20), 1,3-dihydro-