5822-16-2

Upstream product

• 104-86-9 4-chlorobenzylamine 
• 88-73-3 2-Chloronitrobenzene 
• 104-83-6 1-Chloro-4-(chloromethyl)benzene 
• 88-74-4 2-nitro-aniline 
• 1493-27-2 ortho-nitrofluorobenzene 

Downstream Products

• 5729-18-0 N-(p-Chlorophenylmethyl)-2-amino aniline 
• 1019-85-8 2-(4-chlorophenyl)benzimidazole 
• 107456-42-8 1-(4-chlorobenzyl)-1H-benzo[d]imidazole 
• 3689-76-7 Chlormidazole 
• 101103-28-0 chloro-acetic acid-[2-(4-chloro-benzylamino)-anilide] 
• 442-52-4 clemizole 
• 805965-34-8 [1-(4-chloro-benzyl)-1H-benzimidazol-2-ylmethyl]-dimethyl-amine 
• 7189-18-6 1-(4-chlorobenzyl)-2-(chloromethyl)-1H-benzo[d]imidazole 
• 131705-70-9 N-(p-Chlorophenylmethyl)-2(1H)-benzimidazolone 
• 131705-80-1 2-Chloro-1-(p-chlorophenylmethyl)-1H-benzimidazole 

Relevant academic research and scientific papers

CuBr-Catalyzed Oxidation/Coupling: An Efficient and Applicable Strategy for the Synthesis of 2-Aryl Benzimidazoles from 1-Fluoro-2-nitrobenzene and Benzylamines

A novel and efficient route has been developed for the synthesis of benzimidazole derivatives via ligand-free CuBr-catalyzed oxidation and cyclization of 1,2-diamines derived from 1-fluoro-2-nitrobenzene and different arylamines as starting materials. GRAPHICAL ABSTRACT.

Synthesis method of benzimidazole compound based on iron catalytic oxidation-reduction coupling reaction

The invention belongs to the field of organic synthesis, and relates to a benzimidazole compound synthesis method based on an iron catalytic oxidation-reduction coupling reaction. According to the method, o-nitroaniline compounds and alcohol compounds are used as raw materials, and the benzimidazole compounds are generated through iron-catalyzed redox coupling reaction in the presence of an iron catalyst and a proton donor. The method provided by the invention provides a new way for the synthesis of benzimidazole drugs and pesticides. Compared with a traditional benzimidazole compound synthesis method with o-phenylenediamine compounds and carboxylic acid or carboxylic acid derivatives as raw materials, the method has the advantages that the atom utilization rate of the whole process is increased, the production cost is reduced, and waste gas, waste liquid and waste solid generated in the production process is reduced.

BENZIMIDAZOLES AND AZA-BENZIMIDAZOLES, AND METHODS OF USE THEREOF

Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II). (Formulae (II), (III))

3D-Printed Polypropylene Continuous-Flow Column Reactors: Exploration of Reactor Utility in SNAr Reactions and the Synthesis of Bicyclic and Tetracyclic Heterocycles

3D printing has the potential to transform the way in which chemical reactions are carried out due to its low-cost, ease-of-use as a technology and its capacity to expedite the development of iteratively enhanced prototypes. In this present study, we developed a novel, low-cost polypropylene (PP) column reactor that was incorporated into an existing continuous-flow reactor for the synthesis of heterocycles. The utility and solvent resistance of the printed devices were explored in SNAr reactions to produce substituted aniline derivatives and in the synthesis of bicyclic and tetracyclic heterocycles. Using this approach, a range of heterocyclic compounds was synthesised including the core structure of the natural product (±)-γ-lycorane and structurally complex compounds based on the tetracyclic core of the erythrina alkaloids.

Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis

This article describes discovery of a novel and new class of cholinesterase inhibitors as potential therapeutics for Alzheimer's disease. A series of novel isoalloxazine derivatives were synthesized and biologically evaluated for their potential inhibitory outcome for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds exhibited high activity against both the enzymes AChE as well as BuChE. Of the synthesized compounds, the most potent isoalloxazine derivatives (7m and 7q) showed IC50 values of 4.72 μM and 5.22 μM respectively against AChE; and, 6.98 μM and 5.29 μM respectively against BuChE. These two compounds were further evaluated for their anti-aggregatory activity for β-amyloid (Aβ) in presence and absence of AChE by performing Thioflavin-T (ThT) assay and Congo red (CR) binding assay. In order to evaluate cytotoxic profile of these two potential compounds, cell viability assay of SH-SY5Y human neuroblastoma cells was performed. Further, to understand the binding behavior of these two compounds with AChE and BuChE enzymes, docking studies have been reported.

Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists

Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.

DEUTERIUM MODIFIED BENZIMIDAZOLES

This invention relates to derivatives of 1-(p-chIorobenzyI)-2-(1-pyrrolidinylmethyl)benzimidazole according to Formula I wherein at least one Y is deuterium described herein and pharmaceutically acceptable salts thereof. This invention also provides compo

N,N-dialkyl-N′-chlorosulfonyl chloroformamidines in heterocyclic synthesis. Part VII 4-dialkylamino[1,2,3,5]benzoxathiadiazepine dioxides and 4-dialkylamino-[2,1,3,5]benzothiatriazepine dioxides

N,N-dialkyl-N′-chlorosulfonyl chloroformamidines 1 reacted with 2-aminophenols 2 to give 4-dialkylamino[1,2,3,5]benzoxathiadiazepine dioxides 3, which are examples of a new ring system. Reaction of 1 with 1,2-diaminobenzenes 7 afforded 4-dialkylamino[2,1,

A microcapillary system for simultaneous, parallel microwave-assisted synthesis

A continuous flow, microwave-assisted, parallel-capillary microreactor has been developed. Libraries of drug candidates were prepared on the milligram scale with this reactor by injecting plugs of reagents from separate syringes into common reaction capil