612498-85-8

Upstream product

• 99-65-0 meta-dinitrobenzene 
• 81290-20-2 (trifluoromethyl)trimethylsilane 
• 453560-74-2 2-methoxy-4-nitro-1-(trifluoromethyl)benzene 
• 77337-82-7 1-bromo-2-methoxy-4-nitrobenzene 
• 5458-84-4 2-iodo-5-nitroanisole 

Downstream Products

• 1034491-92-3 1-[2-(5-nitro-2-trifluoromethylphenoxy)-ethyl]-pyrrolidine 
• 474953-31-6 1-nitro-3-(2-dimethylamino-ethoxy)-4-trifluoromethylbenzene 
• 769961-18-4 (R)-2-(5-nitro-2-trifluoromethyl-phenoxymethyl)-1-(tert-butylcarbonyl)pyrrolidine 
• 106877-47-8 5-amino-2-trifluoromethylphenol 
• 769960-90-9 (R)-2-((5-isothiocyanato-2-(trifluoromethyl)phenoxy)methyl)-1-methylpyrrolidine 
• 769961-13-9 (R)-3-(1-methyl-pyrrolidin-2-ylmethoxy)-4-trifluoromethyl-phenylamine 
• 769961-28-6 [2-(5-isothiocyanato-2-trifluoromethyl-phenoxy)-ethyl]-dimethyl-amine 
• 474941-22-5 3-(2-dimethylamino-ethoxy)-4-trifluoromethylaniline 
• 952490-88-9 (R)-1-methyl-2-((5-nitro-2-(trifluoromethyl)phenoxy)methyl)-pyrrolidine 
• 952490-85-6 (R)-2-((5-nitro-2-(trifluoromethyl)phenoxy)methyl)-pyrrolidine 

Relevant academic research and scientific papers

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.

Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors

Inhibition of the VEGF signaling pathway has become a valuable approach in the treatment of cancers. Guided by X-ray crystallography and molecular modeling, a series of 2-aminobenzimidazoles and 2-aminobenzoxazoles were identified as potent inhibitors of VEGFR-2 (KDR) in both enzymatic and HUVEC cellular proliferation assays. In this report we describe the synthesis and structure-activity relationship of a series of 2-aminobenzimidazoles and benzoxazoles, culminating in the identification of benzoxazole 22 as a potent and selective VEGFR-2 inhibitor displaying a good pharmacokinetic profile. Compound 22 demonstrated efficacy in both the murine matrigel model for vascular permeability (79% inhibition observed at 100 mg/kg) and the rat corneal angiogenesis model (ED50 = 16.3 mg/kg).

FUSED AZOLES SUCH AS 2,5-DISUBSTITUTED BENZIMIDAZOLES, BENZOXAZOLES AND BENZOTHIAZOLES AS KINASE INHIBITORS

The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.

Oxidative nucleophilic substitution of hydrogen in nitroarenes with trifluoromethyl carbanions. Synthesis of trifluoromethyl phenols

Trifluoromethyl carbanions generated from the Ruppert reagent and TASF add to highly electron-deficient nitroarenes to produce σH adducts subsequently oxidized with dimethyldioxirane to substituted trifluoromethyl phenols.