1396753-41-5

Usage

Molecular structure

The compound contains a benzo[d][1,2,3]triazole ring, a 1-methyl group, and a 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl group.

Usage

The compound is used in organic synthesis and medicinal chemistry as a building block for the development of pharmaceuticals and agrochemicals.

Potential applications

It has been studied for its potential use in optoelectronic and materials science applications.

Functionalization

The dioxaborolane group in the molecule can serve as a versatile handle for further functionalization of the compound.

Value

The compound is a valuable intermediate in the synthesis of diverse chemical entities.

Upstream product

• 364-73-8 4-Bromo-1-fluoro-2-nitrobenzene 
• 944718-31-4 5-bromo-1-methyl-1H-benzo[d][1,2,3]triazole 
• 73183-34-3 bis(pinacol)diborane 
• 53484-26-7 N-methyl-4-bromo-2-nitroaniline 
• 69038-76-2 2-N-methylamino-5-bromoaniline 
• 32046-62-1 5-bromo-1H-benzotriazole 
• 74-88-4 methyl iodide 

Relevant academic research and scientific papers

3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR

The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

SUBSTITUTED QUINOXALINE DERIVATIVES

The present invention relates to substituted quinoxaline derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery

KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress. Pharmacological intervention has focused on molecules that decrease NRF2-ubiquitination through covalent modification of KEAP1 cysteine residues, but such electrophilic compounds lack selectivity and may be associated with off-target toxicity. We report here the first use of a fragment-based approach to directly target the KEAP1 Kelch-NRF2 interaction. X-ray crystallographic screening identified three distinct "hot-spots" for fragment binding within the NRF2 binding pocket of KEAP1, allowing progression of a weak fragment hit to molecules with nanomolar affinity for KEAP1 while maintaining drug-like properties. This work resulted in a promising lead compound which exhibits tight and selective binding to KEAP1, and activates the NRF2 antioxidant response in cellular and in vivo models, thereby providing a high quality chemical probe to explore the therapeutic potential of disrupting the KEAP1-NRF2 interaction.

NRF2 REGULATORS

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.