6567-35-7

Usage

InChI:InChI=1/C4H2BrNO3/c5-3-1-2(4(7)8)9-6-3/h1H,(H,7,8)

Upstream product

• 25742-00-1 (3-bromoisoxazol-5-yl)methanol 
• 105174-97-8 3-Bromo-5-isoxazolecarboxylic Acid Ethyl Ester 
• 272773-11-2 methyl 3-bromoisoxazole-5-carboxylate 
• 1392517-50-8 3-bromo-4,5-dihydro-5-tert-butoxyformylisoxazole 

Downstream Products

• 13626-59-0 3-methoxyisoxazole-5-carboxylic acid 
• 2552-54-7 3-(benzyloxy)isoxazole-5-carboxylic acid 
• 76596-53-7 3-bromo-5-acetyl-isoxazole 
• 1392517-51-9 2-(3-bromoisoxazol-5-yl)-5-(2-trifluoromethylphenyl)-1H-benzimidazole 

Relevant academic research and scientific papers

Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro

The discovery and development of a novel HER-2 tyrosine kinase inhibitor for the treatment of HER2-positive breast cancer are presented in this article. EGFR family has been recognized as a crucial meditator in the cancer progression; HER-2 tyrosine kinase was one of the members among them. In the effort to explore potent HER-2 inhibitors, a novel series of 4-anilino-3-cyanoquinoline derivatives have been designed, synthesized and evaluated. Most compounds possessed modest proliferation inhibition on SK-BR-3 cell line and HER-2 kinase. Compound 16 appeared to be the most potent compound (HER-2 kinase IC50: 19.4?nM, SK-BR-3 IC50: 94?nM). In the experiment of cellular cytotoxicity assay, compound 16 shows a much lower cytotoxicity than neratinib on Beas-2b cell line (Human bronchial epithelial cells). In conclusion, compound 16 would be a promising lead compound for further anti-breast cancer drug discovery.

SUBSTITUTED BENZIMDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS

The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia

Structure-activity studies of 6-substituted decahydroisoquinoline-3- carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity

We have explored the excitatory amino acid antagonist activity in a series of decahydroisoquinoline-3-carboxyic acids, and within this series found the potent and selective AMPA antagonist (3SR,4aRS,6RS,8aRS)-6-(2-(1H-tetrazol- 5-yl)ethyl)decahydroisoquin

Process for the preparation of 3,5-disubstituted isoxazoles

A novel process for the preparation of 3-bromo- and 3-chloro-5-substituted isoxazoles is provided. Dibromo- or dichloro-formaldoxime is reacted with an excess of an 1-alkyne derivative of the formula where R is hydrogen, phenyl or 1-6 C alkyl optionally substituted by halogen, OH, OR', CHO, COR', COOR', CONH2, CONR'R" or NHCOR' where, in turn, R' and R", which may be the same or different, are a 1-6 C alkyl or haloalkyl, in the presence of (i) at least an equimolecular amount, with respect to the dibromo- or dichloro-formaldoxime, of an alkaline base selected from the class consisting of sodium and potassium carbonate and bicarbonate and (ii) an inert solvent in which the 1-alkyne is soluble at room temperature.