7189-72-2

Upstream product

• 621-72-7 2-benzylbenzimidazole 
• 103-82-2 phenylacetic acid 
• 99-56-9 4-Nitrophenylene-1,2-diamine 
• 5442-34-2 ethyl 2-phenylacetimidate hydrochloride 
• 95-54-5 1,2-diamino-benzene 

Downstream Products

• 50832-49-0 (5-nitro-1H-benzo[d]imidazol-2-yl)(phenyl)methanone 
• 33140-62-4 5-Amino-2-(α-hydroxybenzyl)benzimidazole 
• 108281-65-8 N¹,N³-bis-(2-Benzylbenzimidazole-5-yl)urea 
• 108318-61-2 Ethyl 2-Benzyl-1-carboethoxybenzimidazole-5-carbamate 
• 108281-64-7 Methyl 2-Benzyl-1-carbomethoxybenzimidazole-5-carbamate 
• 108281-75-0 Methyl 2-(α-Methoxybenzyl)benzimidazole-5-carbamate 
• 108281-74-9 Methyl 2-(α-Hydroxybenzyl)benzimidazole-5-carbamate 
• 108281-66-9 Ethyl 2-Benzylbenzimidazole-5-carbamate 
• 108281-63-6 Methyl 2-Benzylbenzimidazole-5-carbamate 
• 108281-61-4 2-benzyl-1H-benzo[d]imidazol-5-amine 

Relevant academic research and scientific papers

Targeting Her2-insYVMA with Covalent Inhibitors - A Focused Compound Screening and Structure-Based Design Approach

Mutated or amplified Her2 serves as a driver of non-small cell lung cancer or mediates resistance toward the inhibition of its family member epidermal growth factor receptor with small-molecule inhibitors. To date, small-molecule inhibitors targeting Her2 which can be used in clinical routine are lacking, and therefore, the development of novel inhibitors was undertaken. In this study, the well-established pyrrolopyrimidine scaffold was modified with structural motifs identified from a screening campaign with more than 1600 compounds, which were applied against wild-type Her2 and its mutant variant Her2-A775_G776insYVMA. The resulting inhibitors were designed to covalently target a reactive cysteine in the binding site of Her2 and were further optimized by means of structure-based drug design utilizing a set of obtained complex crystal structures. In addition, the analysis of binding kinetics and absorption, distribution, metabolism, and excretion parameters as well as mass spectrometry experiments and western blot analysis substantiated our approach.

Metal-free aerobic oxidation of benzazole derivatives

2-Benzyl benzothiazoles and benzimidazoles are easily oxidized under air and basic conditions to give the corresponding ketones in good yields. The use of palladium acetate as a catalyst has little effect and even gives, in some cases, much lower yields.

Microwave-assisted synthesis of some novel benzimidazole compounds containing oxadiazole moiety

5(6)-Nitro-2-alkyl/aryl-1H-benzimidazoles were obtained from the reaction of iminoester hydrochlorides and 4-nitro-ophenylenediamine, and converted to their ester and hydrazide derivatives. Hydrazide derivatives were used as a key intermediate to prepare 5-[(2-alkly/arly-5(6)-nitro-1H-benzimidazol-1-yl) methyl]-1, 3, 4-oxadiazol-2-thioles.

Boric acid-catalyzed direct condensation of carboxylic acids with benzene-1,2-diamine into benzimidazoles

The applicability of boric acid catalysis for the direct condensation of carboxylic acids with benzene-1,2-diamine to give 2-substituted benzimidazoles was investigated. It was found that catalytic amounts (5-10 mol-%) of boric acid efficiently promote the cyclocondensation of aliphatic carboxylic acids in refluxing toluene. In addition, the relatively neutral conditions allow the use of acid-sensitive substrates and give rise to specific transformations and selectivities that are not observed with some classical methods. Benzoic acids were found to be less reactive than aliphatic acids and thus require refluxing xylene for better efficiency. Phenylboronic acid was found to be inactive as a catalyst due to its rapid consumption by condensation with benzene-1,2-diamine to give a 2-phenylbenzodiazaborole. Copyright