215115-09-6

Basic information

• Product Name: 8-BROMO-6-METHYL-4-QUINAZOLONE
• Synonyms: 8-BROMO-6-METHYL-4-QUINAZOLONE;8-broMo-6-Methylquinazolin-4-ol;8-BroMo-6-Methylquinazolin-4(3H)-one;8-Bromo-6-methyl-4(1H)-quinazolinone
• CAS NO: 215115-09-6
• Molecular Formula: C₉H₇BrN₂O
• Molecular Weight: 239.07
• Mol File: 215115-09-6.mol
• Article Data: 3

Chemical Properties

• Boiling Point: 378.4±52.0 °C(Predicted)
• Appearance: /
• Density: 1.72±0.1 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Room Temperature
• PKA: 0.43±0.20(Predicted)
• CAS DataBase Reference: 8-BROMO-6-METHYL-4-QUINAZOLONE(CAS DataBase Reference)
• NIST Chemistry Reference: 8-BROMO-6-METHYL-4-QUINAZOLONE(215115-09-6)
• EPA Substance Registry System: 8-BROMO-6-METHYL-4-QUINAZOLONE(215115-09-6)

Safety Data

• Hazardous Substances Data: 215115-09-6(Hazardous Substances Data)

Usage

General Description

8-BROMO-6-METHYL-4-QUINAZOLONE is a chemical compound known for its role as an intermediate in the synthesis of pharmaceuticals. It is used as a building block in the production of various drugs, particularly in the field of medicinal chemistry. 8-BROMO-6-METHYL-4-QUINAZOLONE is characterized by its quinazolone structure, as well as its bromo and methyl substituents, which contribute to its unique chemical properties. 8-BROMO-6-METHYL-4-QUINAZOLONE has potential applications in the development of new drug candidates and has been a subject of interest in pharmaceutical research and development.

Upstream product

• 13091-43-5 2-amino-3-bromo-5-methylbenzoic acid 
• 3473-63-0 formamidine acetic acid 
• 77287-34-4 formamide 

Downstream Products

• 1269421-95-5 4-chloro-N-(2,6-difluoro-3-(propylsulfonamido)phenyl)-6-methylquinazoline-8-carboxamide 
• 1269420-95-2 4-amino-6-methyl-quinazoline-8-carboxylic acid [2,6-difluoro-3-(propane-1-sulfonylamino)-phenyl]-amide 
• 1269420-96-3 4-(cyclopentylamino)-N-(2,6-difluoro-3-(propylsulfonamido)phenyl)-6-methylquinazoline-8-carboxamide 
• 1269421-96-6 4-chloro-N-(2-chloro-6-fluoro-3-(N-(4-methoxybenzyl)(propylsulfonamido))phenyl)-6-methylquinazoline-8-carboxamide 

Relevant articles and documents

Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold

Protease activated receptor 4 (PAR4) is an important target in antiplatelet therapy to reduce the risk of heart attack and thrombotic complications in stroke. PAR4 antagonists can prevent harmful and stable thrombus growth, while retaining initial thrombus formation, by acting on the late diffusion stage of platelet aggregation, and may provide a safer alternative to other antiplatelet agents. To date, only two PAR4 antagonists, BMS-986120 and BMS-986141 have entered clinical trials for thrombosis. Thus, the development of a potent and selective PAR4 antagonist with a novel chemotype is highly desirable. In this study, we explored the activity of quinazolin-4(3H)-one-based PAR4 antagonists, beginning with their IDT analogues. By repeated structural optimisation, we developed a series of highly selective PAR4 antagonists with nanomolar potency on human platelets. Of these, 13 and 30g, with an 8-benzo[d]thiazol-2-yl-substituted quinazolin-4(3H)-one structure, showed optimal activity (h. PAR4-AP PRP IC50 = 19.6 nM and 6.59 nM, respectively) on human platelets. Furthermore, 13 and 30g showed excellent selectivity for PAR4 versus PAR1 and other receptors (IC50s > 10 μM) on human platelets. And 13 and 30g were lack of cross-reactivity for PAR1 or PAR2 (PAR1 AP FLIPR IC50 > 3162 nM, PAR2 AP FLIPR IC50 > 1000 nM) in the calcium mobilization assays. Metabolic stability assays and cytotoxicity tests of 13 and 30g indicated that these compounds could sever as promising drug candidates for the development of novel PAR4 antagonists. In summary, the quinazolin-4(3H)-one-based analogues are the first reported chemotypes with excellent activity and selectivity against PAR4, and, in the current study, we expanded the structural diversity of PAR4 antagonists. The two compounds, 13 and 30g, found in our study could be promising starting points with great potential for further research in antiplatelet therapy.

Substituted Heterocyclic Ethers and Their Use in CNS Disorders

The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.