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Usage

Uses

Used in Pharmaceutical Industry:
2-(pyridin-4-ylmethyl)-1H-benzimidazole is used as a potential active pharmaceutical ingredient for its antitumor properties. It is being studied for its ability to target and inhibit the growth of cancer cells, making it a promising candidate for the development of new anticancer drugs.
Used in Agrochemical Industry:
2-(pyridin-4-ylmethyl)-1H-benzimidazole is used as a potential active ingredient in agrochemicals for its antimicrobial properties. It is being investigated for its ability to combat various microbial pathogens that can harm crops, potentially leading to the creation of new pesticides or fungicides.
Used in Medicinal Chemistry Research:
2-(pyridin-4-ylmethyl)-1H-benzimidazole is used as a valuable tool in medicinal chemistry research. Its unique structure and properties make it a useful compound for studying the mechanisms of action of various biological activities, such as its antitumor and antimicrobial effects.
Used in Drug Development:
2-(pyridin-4-ylmethyl)-1H-benzimidazole is used as a building block in drug development. Its potential as a precursor for the synthesis of various pharmaceuticals and agrochemicals makes it an important compound for the creation of new and improved drugs.

Upstream product

• 29800-89-3 methyl 4-pyridineacetate 
• 95-54-5 1,2-diamino-benzene 
• 54401-85-3 pyridin-4-yl-acetic acid ethyl ester 
• 6622-91-9 2-(pyridine-4-yl)acetic acid hydrochloride 

Relevant academic research and scientific papers

Fragment-based discovery of 7-azabenzimidazoles as potent, highly selective, and orally active CDK4/6 inhibitors

Herein, we describe the discovery of potent and highly selective inhibitors of both CDK4 and CDK6 via structure-guided optimization of a fragment-based screening hit. CDK6 X-ray crystallography and pharmacokinetic data steered efforts in identifying compound 6, which showed >1000-fold selectivity for CDK4 over CDKs 1 and 2 in an enzymatic assay. Furthermore, 6 demonstrated in vivo inhibition of pRb-phosphorylation and oral efficacy in a Jeko-1 mouse xenograft model.

A series of alkaline earth metal coordination polymers constructed from two newly designed imidazole-based dicarboxylate ligands containing pyridinylmethyl groups

Two new imidazole-based dicarboxylate ligands, which are 2-(pyridin-4-ylmethyl)-1H-imidazole-4,5-dicarboxylic acid (H3pPyMIDC) and 2-(pyridin-3-ylmethyl)-1H-imidazole-4,5-dicarboxylic acid (H3mPyMIDC), have been designed and successfully synthesized. Both these multidentate ligands are then used to react with different kinds of alkaline earth metal ions under solvothermal conditions, leading to the construction of a series of new coordination polymers (CPs), namely, [Ba(μ5-HpPyMIDC)(H2O)]n (1), [Sr(μ5-HpPyMIDC)(H2O)]n (2), [Ca2(μ4-HpPyMIDC)2(H2O)2]n (3), {[Ca2(μ3-HpPyMIDC)(μ4-HpPyMIDC)(H2O)2]·H2O}n (4), [Ba(μ5-HmPyMIDC)(H2O)]n (5), {[Mg10(μ3-mPyMIDC)3(μ4-mPyMIDC)3(H2O)21]·SO4·12H2O}n (6) and {[Sr(μ2-H2mPyMIDC)2(DMF)2]n·H2O}n (7). Compounds 1 and 2 are isostructural, exhibiting two-dimensional (2D) network structures with a hexagonal honeycomb (6,3) topology if the corresponding metal ions are seen as 3-connected nodes. Compound 3 displays another type of 2D network, which is built by the connection of μ4-HpPyMIDC ligands and Ca(ii) centres. Compound 4 is a binodal (3,4)-connected 3D framework with the Schl?fli symbol of (6·82)(65·8). The 2D structure of compound 5 is similar to those of compounds 1 and 2, although different kinds of ligands are employed. Compound 6 exhibits an interesting 3D framework with a pcu topology by considering each unusual heptanuclear magnesium cluster as a 6-connected node. In compound 7, connection of μ2-H2mPyMIDC ligands with Sr(ii) ions results in the formation of an uncommon 3D chiral framework containing two different types of 1D helical chains. The present results reveal that both these new imidazole-based dicarboxylate ligands containing flexible pyridinylmethyl groups show versatile coordination abilities and are good candidates for fabricating new CPs. Moreover, the thermogravimetric and solid-state luminescence properties of all the compounds have also been studied.

TNF -Alpha Modulating Benzimidazoles

A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

An advantageous synthesis of 2-substituted benzimidazoles using polyphosphoric acid. 2-(pyridyl)-1H-benzimidazoles, 1-alkyl-(1H-benzimidazol-2-yl)pyridinium salts, their homologues and vinylogues

The title 2-substituted benzimidazoles are prepared by a highly efficient one-pot procedure, cyclodehydration of the corresponding accessible carboxylic acids and 1,2-arylenediamines, using polyphosphoric acid as the catalyst and solvent in a condensation of the type found in the Phillips benzimidazole synthesis. The method has been adapted and proved to be extremely useful for 1-alkyl-(1H-benzimidazol-2-yl)pyridinium tetrafluoroborates with a methylene and vinylene interannular moiety.

Practicable Syntheses of 2-Hydroxymethyl-substituted Benzimidazoles and 2-Formylbenzimidazole

N-Protection of benzimidazole by a diethoxymethyl group, as in , allows exclusive lithiation at the 2-position.This protected anion can be made to react with various electrophiles (e. g. ketones, aldehydes) to yield the corresponding 2-hydroxymethylbenzimidazoles (1).Facile deprotection occurs with acid.Two practicable syntheses of 2-formylbenzimidazole are also described and an indirect route to benzimidazole-2-alcohols is discussed.