66504-19-6

Upstream product

• 74426-51-0 4-(trifluoromethyl)phenylacetyl chloride 
• 32857-62-8 4-Trifluoromethylphenylacetic acid 
• 721-63-1 (4-trifluoromethylphenyl)acetic acid ethyl ester 

Downstream Products

• 721-63-1 (4-trifluoromethylphenyl)acetic acid ethyl ester 

Relevant academic research and scientific papers

SUBSTITUTED PIPERAZINE DERIVATIVES USEFUL AS T CELL ACTIVATORS

Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R4, R5, R6, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions

Nuclear factor erythroid 2-related factor 2 (NRF2) is a pleiotropic transcription factor which regulates the constitutive and inducible transcription of a wide array of genes and confers protection against a variety of pathologies. Directly disrupting Kelch-like ECH-associated protein 1 (KEAP1)-NRF2 protein-protein interaction (PPI) has been explored as a promising strategy to activate NRF2. We reported here the first identification of a series of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 inhibitors. Our efforts led to the potent small molecule KEAP1-NRF2 inhibitor, 20c, which exhibited a Kd of 24 nM to KEAP1 and an IC50 of 75 nM in disrupting KEAP1-NRF2 interaction. Subsequent biological studies provided consistent evidence across mouse macrophage cell-based and in vivo models that 20c induced NRF2 target gene expression and enhanced downstream antioxidant and anti-inflammatory activities. Our study not only demonstrated that small molecule KEAP1-NRF2 PPI inhibitors can be potential preventive and therapeutic agents for diseases and conditions involving oxidative stress and inflammation but also enriched the chemical diversity of the KEAP1-NRF2 inhibitors.

Bromination of α-Diazo Phenylacetate Derivatives Using Cobalt(II) Bromide

A method for the bromination of α-diazo phenylacetate derivatives using cobalt(II) bromide is described. This bromination reaction features a short reaction time, broad substrate scope, operational simplicity, acid-free conditions, and gram-scalability. (Figure presented.).

Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia

We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia. In order to mitigate the concerns for potential systemic side effects, we

INHIBITORS OF HIF PROLYL HYDROXYLASE

The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Growth hormone secretagogues

What is disclosed are growth hormone secretagogues, and their uses, of the formula wherein R1 is C6H5CH2OCH2—, C6H5(CH2)3— or indol-3-ylmethyl; Y is pyrrolidin-1-yl, 4-C1-C6alkylpiperidin-1-yl or NR2R2; R2 are each independently a C1to C6alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6alkoxy or phenyl; and R4 is H or CH3, or a pharmaceutically acceptable salt or solvate thereof.

Electrochemistry of Ethyl α-Bromo-α-fluoro(phenyl)acetate and some Ethyl α-Bromo(trifluoromethylphenyl)acetates and Electrochemical Synthesis of the Corresponding Diastereoisomeric Diethyl Succinates.

Ethyl α-bromoesters (1)-(5) (ABr) were prepared through NBS bromination of (6)-(10) (AH) respectively.Controlled potential electrolysis of (1)-(5), dissolved in dry dimethylformamide (DMF) containing Et4NClO4 (0.1 M) allows the corresponding succinates (1