1129541-62-3

Usage

Uses

Used in Pharmaceutical Industry:
4-(3-Bromo-5-fluorophenyl)morpholine is used as a pharmaceutical intermediate for its antiviral, antimicrobial, and anticancer properties. It serves as a key building block in the synthesis of potential drug candidates and bioactive compounds, contributing to the development of novel therapeutic agents.
Used in Organic Synthesis:
In the field of organic synthesis, 4-(3-Bromo-5-fluorophenyl)morpholine is utilized as a valuable intermediate for the production of various biologically active compounds. Its unique structural features allow for the creation of new molecules with potential applications in medicine and other industries.
Used in Drug Development:
4-(3-Bromo-5-fluorophenyl)morpholine is employed in drug development as a precursor for the synthesis of innovative pharmaceuticals. Its presence in the molecular structure of drug candidates can enhance their therapeutic efficacy and selectivity, leading to improved treatment options for various diseases and conditions.

Upstream product

• 110-91-8 morpholine 
• 461-96-1 3,5-difluorobromobenzene 
• 5414-19-7 1,1'-oxybis(2-bromo-ethane) 
• 134168-97-1 3-bromo-5-fluoroaniline 

Downstream Products

• 1129541-03-2 4-(3-fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)morpholine 

Relevant academic research and scientific papers

METTL3 INHIBITORY COMPOUNDS

The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z5 (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity 10 is implicated.

Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors

Given the significant body of data supporting an essential role for c-jun-N-terminal kinase (JNK) in neurodegenerative disorders, we set out to develop highly selective JNK inhibitors with good cell potency and good brain penetration properties. The structure-activity relationships (SAR) around a series of aminopyrimidines were evaluated utilizing biochemical and cell-based assays to measure JNK inhibition and brain penetration in mice. Microsomal stability in three species, P450 inhibition, inhibition of generation of reactive oxygen species (ROS), and pharmacokinetics in rats were also measured. Compounds 9g, 9i, 9j, and 9l had greater than 135-fold selectivity over p38, and cell-based IC50 values 50 = 0.8 nM for inhibition of ROS and had good pharmacokinetic properties in rats along with a brain-to-plasma ratio of 0.75. These results suggest that biaryl substituted aminopyrimidines represented by compound 9l may serve as the first small molecule inhibitors to test efficacy of JNK inhibitors in neurodegenerative disorders. 2009 American Chemical Society.