38191-34-3

Usage

Chemical Properties

white to light yellow solid

InChI:InChI=1/C6H6BrNO/c7-4-1-2-5(8)6(9)3-4/h1-3,9H,8H2

Upstream product

• 19932-85-5 6-bromobenzo[d]oxazol-2(3H)-one 
• 2101-88-4 1-azido-4-bromobenzene 
• 7664-93-9 sulfuric acid 
• 10468-46-9 N-(4-bromophenyl)hydroxylamine 
• 591-20-8 3-Bromophenol 
• 106-40-1 4-bromo-aniline 
• 95-55-6 2-amino-phenol 
• 5683-43-2 2-methyl-6-nitrobenzoxazole 
• 5676-60-8 6-amino-2-methylbenzoxazole 
• 16394-40-4 N-(4-bromo-2-hydroxyphenyl)acetamide 
• 441019-63-2 2-amino-5-bromophenyl sulphate 
• 27684-84-0 5-bromo-2-nitrophenol 

Downstream Products

• 858855-11-5 5-bromo-2-iodo-phenol 
• 855246-05-8 1-benzoylamino-2-benzoyloxy-4-bromo-benzene 
• 872287-84-8 4-bromo-2-hydroxy-benzenediazonium betaine 
• 96462-69-0 N-(4-bromo-2-hydroxy-phenyl)-N'-(3,4-dichloro-phenyl)-urea 
• 24316-84-5 6-Brombenzoxazolinthion 
• 126190-16-7 Dithiocarbonic acid S-(4-bromo-2-hydroxy-phenyl) ester O-ethyl ester 
• 126260-52-4 2-{[4-Bromo-2-(toluene-4-sulfonyloxy)-phenyl]-hydrazono}-propionic acid ethyl ester 
• 537025-33-5 6-bromo-2-phenylbenzo[d]oxazole 
• 537029-51-9 6-bromo-2-(4-chlorobenzyl)benzoxazole 
• 321436-06-0 7-bromo-3,4-dihydro-2H-1,4-benzoxazin-3-one 
• 116632-17-8 2-amino-3,5-dibromo-phenol 
• 1333317-65-9 8-benzyloxy-6-bromo-4-methylquinoline 
• 1333317-66-0 8-benzyloxy-6-cyano-4-methylquinoline 
• 1413929-84-6 C₁₄H₁₁BrClNO₂S 

Relevant academic research and scientific papers

HMOX1 inducers

The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.

Synthesis of benzoxazoles via the copper-catalyzed hydroamination of alkynones with 2-aminophenols

We describe herein the synthetic method to benzoxazole derivatives via the copper-catalyzed hydroamination of alkynones with 2-aminophenols. The method produced a wide variety of functionalized benzoxazole derivatives in good yields. Preliminary mechanistic experiments revealed that the reaction would proceed through the copper-catalyzed hydroamination of alkynones and the sequential intramolecular cyclization of β-iminoketones/elimination of acetophenone promoted by the copper catalyst.

One-Pot Protocol to Synthesize 2-Aminophenols from Anilines via Palladium-Catalyzed C-H Acetoxylation

This paper describes a facile one-pot protocol to synthesize 2-aminophenol derivatives via a palladium-catalyzed C-H acetoxylation strategy with 5-nitropyrimidine as a directing group (DG), which can be easily preinstalled and readily removed under mild condition after the coupling. In addition, the transformation is operationally simple, has high functional group tolerance, and is amenable to gram-scale. Moreover, several examples were shown that introduction/removal of 5-nitropyrimidine and the C-H oxylation sequence could be integrated in one pot.

Ortho-aminophenol derivative and preparation method thereof

The invention first discloses a preparation method of an ortho-aminophenol derivative. The preparation method comprises the following steps: (1) by adopting an aryl amine compound as a substrate and 2-chloro-5-nitropyridine as a guiding base, reacting in acetonitrile, thus obtaining a pyridine aryl amine compound intermediate; (2) catalyzing the pyridine aryl amine compound intermediate in step (1) to make C-H activation reaction in a solvent by using iodobenzene diacetate as an oxidant and palladium acetate as a catalyst, thus obtaining an acetoxylation aniline derivative, draining, and thenperforming the chromatographic separation and purification; and (3) enabling the acetoxylation aniline derivative in step (2) to react in a tetrahydrofuran solvent for 30 min at a normal temperature by virtue of hydrazine hydrate, thus obtaining the ortho-aminophenol derivative, quenching, washing, extracting, drying, draining, and performing the chromatographic separation and purification. The invention also discloses the ortho-aminophenol derivative prepared by the method.

SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS

The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. wherein, ring D is Formula (a) or Formula (b): A and B, which may be same or different, are independently CR3 or N; Y is CR3 or N; L is selected from —NR2C(O)—, —C(O)NR2— and —NR2CRaRb—; Ra and Rb are independently hydrogen, halogen or substituted or unsubstituted alkyl; ring E is selected from the Formula (i) to (vii).

Enhanced treatment regimens using mTor inhibitors

The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.

Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formation assay.

COMBINATION OF KINASE INHIBITORS AND USES THEREOF

The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.

COMBINATION PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

The present invention provides for methods and pharmaceutical compositions for treating proliferative disorders. In one aspect, the method comprises administration of two cell-cycle suppressors having a synergistic effect. In another aspect, two cell-cycle suppressors having a synergistic effect are provided in a pharmaceutical composition.