1262859-92-6

Basic information

• Product Name: 4-bromo-1-fluoro-2-nitromethyl-benzene
• Synonyms: 4-bromo-1-fluoro-2-nitromethyl-benzene
• CAS NO: 1262859-92-6
• Molecular Weight: 234.025
• Mol File: 1262859-92-6.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: 4-bromo-1-fluoro-2-nitromethyl-benzene(CAS DataBase Reference)
• NIST Chemistry Reference: 4-bromo-1-fluoro-2-nitromethyl-benzene(1262859-92-6)
• EPA Substance Registry System: 4-bromo-1-fluoro-2-nitromethyl-benzene(1262859-92-6)

Safety Data

• Hazardous Substances Data: 1262859-92-6(Hazardous Substances Data)

Upstream product

• 99725-12-9 4-bromo-2-(bromomethyl)-1-fluorobenzene 
• 93777-26-5 5-bromo-2-fluorobenzaldehyde 

Downstream Products

• 1262859-93-7 2-(5-bromo-2-fluoro-phenyl)-2-nitro-propane-1,3-diol 
• 1429870-22-3 5-[5-(4-bromo-2-chloro-benzylamino)-2-fluoro-phenyl]-5-fluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-ylamine 
• 1429869-80-6 {5-[5-(4-bromo-2-chloro-benzylamino)-2-fluoro-phenyl]-5-fluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-yl}-carbamic acid tert-butyl ester 
• 1262859-98-2 [5-(5-amino-2-fluoro-phenyl)-5-fluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-yl]-carbamic acid tert-butyl ester 

Relevant articles and documents

Organocatalytic, diastereo- and enantioselective synthesis of nonsymmetric cis -stilbene diamines: A platform for the preparation of single-enantiomer cis -imidazolines for protein-protein inhibition

The finding by scientists at Hoffmann-La Roche that cis-imidazolines could disrupt the protein-protein interaction between p53 and MDM2, thereby inducing apoptosis in cancer cells, raised considerable interest in this scaffold over the past decade. Initial routes to these small molecules (i.e., Nutlin-3) provided only the racemic form, with enantiomers being enriched by chromatographic separation using high-pressure liquid chromatography (HPLC) and a chiral stationary phase. Reported here is the first application of an enantioselective aza-Henry approach to nonsymmetric cis-stilbene diamines and cis-imidazolines. Two novel mono(amidine) organocatalysts (MAM) were discovered to provide high levels of enantioselection (>95% ee) across a broad range of substrate combinations. Furthermore, the versatility of the aza-Henry strategy for preparing nonsymmetric cis-imidazolines is illustrated by a comparison of the roles of aryl nitromethane and aryl aldimine in the key step, which revealed unique substrate electronic effects providing direction for aza-Henry substrate-catalyst matching. This method was used to prepare highly substituted cis-4,5-diaryl imidazolines that project unique aromatic rings, and these were evaluated for MDM2-p53 inhibition in a fluorescence polarization assay. The diversification of access to cis-stilbene diamine-derived imidazolines provided by this platform should streamline their further development as chemical tools for disrupting protein-protein interactions.

Oxazine Derivatives and their Use in the Treatment of Neurological Disorders

The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.

OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.