129409-55-8

Upstream product

• 64-17-5 ethanol 
• 658-99-1 (3,4-difluorophenyl)acetonitrile 
• 129409-53-6 ethyl α-bromo-3,4-difluorophenylacetate 
• 658-93-5 (3,4-difluorophenyl)acetic acid 
• 121639-61-0 3,4-difluorophenylacetyl chloride 
• 454-31-9 ethyl difluoroacetate 

Downstream Products

• 129409-53-6 ethyl α-bromo-3,4-difluorophenylacetate 
• 405196-49-8 2-(3,4-difluorophenyl)pentanedioic acid 5-(1,1-dimethylethyl)-1-ethyl ester 
• 131505-78-7 diethyl (3,4-difluorophenyl)propanedioate 
• 286440-92-4 2-(3,4-difluorophenyl)ethan-1-ol 
• 109346-84-1 2-(3,4-difluorophenyl)acetaldehyde 
• 1072429-37-8 [1,1] 2-(3,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 
• 1363145-33-8 ethyl 8-(3,4-difluorophenyl)-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine-8-carboxylate 
• 1363145-28-1 ethyl 3-(3,4-difluorophenyl)-2-(methylsulfanyl)-3,4,5,6-tetrahydropyridine-3-carboxylate 
• 1363144-48-2 ethyl 8-(3,4-difluorophenyl)-3-[3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine-8-carboxylate 
• 1363144-43-7 ethyl 3-(3,4-difluorophenyl)-2-thioxopiperidine-3-carboxylate 
• 1363144-39-1 ethyl 3-(3,4-difluorophenyl)-2-oxopiperidine-3-carboxylate 
• 1363144-34-6 diethyl (2-cyanoethyl)(3,4-difluorophenyl)propanedioate 
• 1363134-56-8 2-{8-(3,4-difluorophenyl)-3-[3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-8-yl}propan-2-ol 
• 129430-64-4 meso-diethyl 2,3-bis(3,4-difluorophenyl)succinate 

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.

Preparation of Organic Nitrates from Aryldiazoacetates and Fe(NO3)3·9H2O

A thermal protocol is reported for the formal insertion of nitric acid into aryldiazoacetates using Fe(NO3)3·9H2O. This strategy is mild and high yielding and allows the preparation of a large variety of members of an unprecedented family of organic nitrates. The nitrate group can be also readily transformed into other functional groups and heterocyclic moieties and can possibly allow new biological explorations of untapped potential associated with their NO-releasing ability.

3,3-DIFLUORO-PIPERIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS

Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).

HETEROCYCLIC COMPOUND AND USE THEREOF

The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.

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.