1282516-66-8

Usage

Uses

Used in Pharmaceutical Research:
5-bromo-2-(1H-imidazol-2-yl)phenol is used as a key intermediate in the synthesis of various pharmaceutical compounds, particularly those targeting the central nervous system. Its unique structure allows for the development of drugs with potential therapeutic applications in treating neurological disorders and conditions.
Used in Organic Synthesis:
As a chemical compound with a bromine atom and an imidazole ring, 5-bromo-2-(1H-imidazol-2-yl)phenol is used as a versatile building block in organic synthesis. It can be employed in the preparation of a wide range of organic molecules, including those with potential applications in various industries.
Used in Drug Discovery:
5-bromo-2-(1H-imidazol-2-yl)phenol is used as a lead compound in drug discovery efforts. Its biological activities, such as potential anti-inflammatory and anti-cancer properties, make it a promising candidate for the development of novel therapeutic agents. Researchers can use 5-broMo-2-(1H-iMidazol-2-yl)phenol as a starting point to design and optimize new drugs with improved efficacy and safety profiles.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 5-bromo-2-(1H-imidazol-2-yl)phenol is used as a valuable tool for understanding the structure-activity relationships of various biologically active molecules. Its unique structural features can provide insights into the design of more effective and selective drugs, ultimately contributing to the advancement of pharmaceutical research.
Used in Anti-inflammatory and Anti-cancer Research:
5-bromo-2-(1H-imidazol-2-yl)phenol is used as a potential therapeutic agent in anti-inflammatory and anti-cancer research. Its biological activities suggest that it may have the ability to modulate inflammatory processes and inhibit the growth and progression of cancer cells. Further studies are needed to fully understand its mechanisms of action and optimize its potential as a treatment for these conditions.

Upstream product

• 131543-46-9 Glyoxal 
• 22532-62-3 4-bromosalicylaldehyde 
• 591-20-8 3-Bromophenol 

Downstream Products

• 1401300-81-9 2-(2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)benzenesulfonamide 
• 2060571-02-8 (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide 
• 1282512-48-4 taselisib 
• 1282516-74-8 9-bromo-5,6-dihydrobenzo[f]imidazo[1,2-d]-[1,4]oxazepine-2-carboxylic acid 
• 1282516-68-0 9-bromo-2,3-diiodo-5,6-dihydrobenzo[f ]imidazo[1,2-d][1,4]oxazepine 

Relevant academic research and scientific papers

INHIBITOR CONTAINING TRICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

An inhibitor containing a tricyclic derivative, a preparation method therefor and a pharmaceutical composition comprising the inhibitor, as well as a use thereof as a phosphoinositide 3 kinase (PI3K) inhibitor in the treatment of cancer and diseases or conditions mediated by or dependent on PI3K imbalance.

Crystal form containing triple-fused-ring derivative free alkali and pharmaceutical composition thereof

The invention relates to a crystal form containing triple-fused-ring derivative free alkali and a pharmaceutical composition thereof. The invention specifically relates to a crystal form of a compound free alkali with a general formula (I), a preparation method, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and an application of the crystal form in preparation of drugs for treating PI3K-mediated related diseases.

Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 1: Early-Stage Development Routes to the Bromobenzoxazepine Core

Two convergent regioselective routes for the synthesis of the tetracyclic imidazobenzoxazepine triazole 1, a key intermediate toward the synthesis of taselisib, are described. In the first-generation route, a chemoselective Negishi cross-coupling reaction was developed between iodoimidazole 3 and triazole 7, which enabled the delivery of initial kilogram quantities of 1. Because of the inefficiencies in the preparation of the imidazole 3, a second-generation route via a highly regioselective imidazole ring formation between α-chloroketone 11 and aryl amidine 12 was developed. The resulting imidazole 14 provided the handle to efficiently install the seven-membered benzoxazepine ring system in one pot with two-step N-alkylation and SNAr tandem reactions.

BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE

Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide- 3 kinase (PI3K) modulation activity or function having the Formula (I) structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE

Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

Fused tricyclic hepatitis virus inhibitor and application thereof

The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d ][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2- methylpropanamide (GDC-0032): A β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity

Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin PI3K inhibitors, we observed a strong dependency of in vivo antitumor activity on the free-drug exposure. By lowering the intrinsic clearance, we derived a set of imidazobenzoxazepin compounds that showed improved unbound drug exposure and effectively suppressed growth of tumors in a mouse xenograft model at low drug dose levels. One of these compounds, GDC-0032 (11l), was progressed to clinical trials and is currently under phase I evaluation as a potential treatment for human malignancies.

BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE

Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.