839715-01-4

Usage

Uses

Used in Pharmaceutical Synthesis:
Tert-butyl (3-bromo-4-(trifluoromethoxy)phenyl)carbamate is used as an intermediate in the synthesis of pharmaceuticals for its potential to contribute to the development of new drugs. Its unique structure allows for the creation of molecules with specific biological activities, making it a valuable component in medicinal chemistry.
Used in Agrochemical Production:
In the agrochemical industry, tert-butyl (3-bromo-4-(trifluoromethoxy)phenyl)carbamate is utilized as a building block in the production of various agrochemicals. Its properties may contribute to the creation of compounds with pesticidal or herbicidal activities, enhancing crop protection and yield.
Used in Organic Compounds Synthesis:
Tert-butyl (3-bromo-4-(trifluoromethoxy)phenyl)carbamate is also used in the synthesis of other organic compounds. Its reactivity and structural features make it a suitable candidate for the formation of complex organic molecules, which can be applied in various chemical and industrial processes.
Used in Medicinal Chemistry and Drug Discovery:
Due to its unique structure and properties, tert-butyl (3-bromo-4-(trifluoromethoxy)phenyl)carbamate has potential applications in medicinal chemistry and drug discovery. It may exhibit biological activities and interactions that warrant further research and investigation, potentially leading to the development of novel therapeutic agents.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 191602-54-7 3-bromo-4-(trifluoromethoxy)aniline 

Downstream Products

• 839715-02-5 [3-(2-methyl-2H-pyrazol-3-yl)-4-trifluoromethoxyphenyl]carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2, 4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine 2A Inverse Agonists for the Treatment of Insomnia

Insomnia affects a growing portion of the adult population in the U.S. Most current therapeutic approaches to insomnia primarily address sleep onset latency. Through the 5-hydroxytryptamine2A (5-HT2A) receptor, serotonin (5-HT) plays a role in the regulation of sleep architecture, and antagonists/ inverse-agonists of 5-HT2A have been shown to enhance slow wave sleep (SWS). We describe here a series of 5-HT2A inverse-agonists that when dosed in rats, both consolidate the stages of NREM sleep, resulting in fewer awakenings, and increase a physiological measure of sleep intensity. These studies resulted in the discovery of 1-[3-(4-bromo-2- methyl-2i/-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin), a potent inverse-agonist of 5-HT2A that was advanced into clinical trials for the treatment of insomnia.

BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C

A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO2-, -CO-, -NR′-CO-NR′′-, -NR′-S(O)2-, -S(O)2-NR′-, -SO2-, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C1-C2 alkylene)-NR′- or -(C1-C2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C1-C4 alkyl; - R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′ , -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents -CO-, -SO- or -S(O)2-; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -(C1-C4 alkyl)-X1, -CO2R′, -SO2NR′R′′, -S(O)2-R′, -CONR′R′′, -NR′-CO-R′′′, -NR′-S(O)2-R′′′, -CO-NR′-(C1-C4 alkyl)-NR′R′′ and -CO-O-(C1-C4 alkyl)-NR′R′′ and/or (b) 1, 2 or 3 unsubstituted substituents selected from -(C1-C4 alkyl)-X2, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 hydroxyalkyl, hydroxy, cyano, nitro and -NR′R′′, wherein X1 is -CO2R′, -SO2-R′, -NR′-CO2-R′′, -NR′-S(O)2-R′′′, -CONR′R′′ or -SO2-NR′R′′, each X2 is the same or different and is cyano, nitro or -NR′R′′, each R′ and R′′ is the same or different and represents hydrogen or C1-C4 alkyl and each R′′′ is the same or different and represents C1-C4 alkyl.

DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERTO

The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to