129409-54-7

Upstream product

• 129409-52-5 ethyl α-bromo-2,4-difluorophenylacetate 
• 64-17-5 ethanol 
• 81228-09-3 2,4-difluorophenylacetic acid 

Downstream Products

• 894789-39-0 C₁₀H₉F₂NO₃ 
• 157372-95-7 ethyl 2-(2,4-difluorophenyl)-2-oxoacetate 
• 129430-60-0 meso-diethyl 2,3-bis(2,4-difluorophenyl)succinate 
• 129409-52-5 ethyl α-bromo-2,4-difluorophenylacetate 
• 1588424-03-6 7-chloro-3-(2,4-difluorophenyl)-1-ethyl-1,6-naphthyridin-2(1H)-one 

Relevant academic research and scientific papers

2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists

A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor.

Identification and Profiling of Hydantoins - A Novel Class of Potent Antimycobacterial DprE1 Inhibitors

Tuberculosis is the leading cause of death worldwide from infectious diseases. With the development of drug-resistant strains of Mycobacterium tuberculosis, there is an acute need for new medicines with novel modes of action. Herein, we report the discovery and profiling of a novel hydantoin-based family of antimycobacterial inhibitors of the decaprenylphospho-β-d-ribofuranose 2-oxidase (DprE1). In this study, we have prepared a library of more than a 100 compounds and evaluated them for their biological and physicochemical properties. The series is characterized by high enzymatic and whole-cell activity, low cytotoxicity, and a good overall physicochemical profile. In addition, we show that the series acts via reversible inhibition of the DprE1 enzyme. Overall, the novel compound family forms an attractive base for progression to further stages of optimization and may provide a promising drug candidate in the future.

MULTIPLE KINASE PATHWAY INHIBITORS

Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.

Process for the preparation of fluorophenylalkylene acid derivatives

The invention relates to the preparation of fluorophenylalkylene acid derivatives of the formulae (4-1)-(4-3): by reaction between fluoroarylmetal halides of formulae (1-1) or (1-2) with carboxylic acid derivatives of formulae (2-1)-(2-3): in the presence

Electrochemistry of some Ethyl α-Bromo(Dihalophenyl) Acetates and Electrochemical Synthesis of Diastereoisomeric Diethyl 2,3-Bis(dihalogenophenyl)Succinates

Ethyl α-bromo-2,4- or -3,4-dihalogenophenylacetates (ABr), where halogen = F or Cl, are prepared and electrolysed on reticulated vitreous carbon (RVC) in dimethylformamide containing Et4NClO4 (0.1 mol dm-3).Potentiostatic reduction at E = -1.6 to -1.8 V versus SCE furnishes the corresponding racemic and meso succinates (AA) (13)-(16).Monoesters AH (5)-(8) are also isolated.An excess of racemic isomer is observed for (14), (15), and (16).Voltammetric experiments show practically no difference between the reduction potentials of the isomeric compounds.Diastereoisomers can be distinguished by NMR spectroscopy, allowing diastereoisomeric excess (de) to be evaluated before isolation of the single products.A mechanism involving radical intermediates A* cannot be excluded.On this basis, the des can be explained by assuming different geometries for A* when the phenyl group bears different substituents.