1232505-74-6

Basic information

• Product Name: 2-fluoro-5-methoxy-4-methylphenylamine
• Synonyms: 2-fluoro-5-methoxy-4-methylphenylamine
• CAS NO: 1232505-74-6
• Molecular Weight: 155.172
• Mol File: 1232505-74-6.mol

Chemical Properties

• CAS DataBase Reference: 2-fluoro-5-methoxy-4-methylphenylamine(CAS DataBase Reference)
• NIST Chemistry Reference: 2-fluoro-5-methoxy-4-methylphenylamine(1232505-74-6)
• EPA Substance Registry System: 2-fluoro-5-methoxy-4-methylphenylamine(1232505-74-6)

Safety Data

• Hazardous Substances Data: 1232505-74-6(Hazardous Substances Data)

Upstream product

• 134882-63-6 1-fluoro-4-methoxy-5-methyl-2-nitro-benzene 

Downstream Products

• 1262897-93-7 N-(2-fluoro-5-methoxy-4-methylphenyl)-3,3-dimethylbutyramide 
• 1262898-01-0 4-(3,3-dimethylbutyrylamino)-5-fluoro-2-methoxybenzoic acid 
• 1262897-90-4 4-(3,3-dimethylbutyrylamino)-5-fluoro-2-methoxy-N-thiazol-2-ylbenzamide 
• 1232688-44-6 1-fluoro-2-isocyanato-4-methoxy-5-methyl-benzene 

Relevant articles and documents

Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)- 3,5-difluorobenzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A phosphonooxymethylene prodrug of a potent and selective hA2A receptor antagonist

The discovery and structure-activity relationship of a series of hA 2A receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson's disease. It had acceptableADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage. As a consequence, prodrugs of 28 were prepared with dramatically increased aqueous solubility. The prodrugs efficiently delivered 28 into systemic circulation, with no detectable levels of prodrug in plasma samples. From this investigation, we selected 32 (Lu AA47070), a phosphonooxymethylene prodrug of 28, as a drug candidate.

DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

DIHYDROPYRIDONE AMIDESAS P2X7 MODULATORS

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.