453560-64-0

Upstream product

• 1448037-95-3 C₁₃H₂₀N₄O₃ 
• 124898-13-1 trimethyl(pentafluoroethyl)silane 
• 354-64-3 Pentafluoroethyl iodide 
• 5458-84-4 2-iodo-5-nitroanisole 

Downstream Products

• 453560-63-9 5-nitro-2-pentafluoroethylphenol 
• 769961-25-3 (R)-1-methyl-2-(5-amino-2-pentafluoroethyl-phenoxymethyl)-pyrrolidine 
• 952490-89-0 (R)-1-methyl-2-(5-nitro-2-pentafluoroethyl-phenoxymethyl)-pyrrolidine 
• 952490-86-7 (R)-2-(5-nitro-2-pentafluoroethyl-phenoxymethyl)-pyrrolidine 
• 952490-83-4 (R)-2-(5-nitro-2-pentafluoroethyl-phenoxymethyl)-1-(tert-butylcarbonyl)pyrrolidine 

Relevant academic research and scientific papers

Trifluoromethylation of 1-aryl-3,3-diisopropyltriazenes

A new method for the trifluoromethylation of functionalized aromatic diisopropyltriazenes is described. In a facile two-step, one-pot synthesis, various functionalized trifluoromethyl-substituted arenes are accessible in mostly good yields by using methyl iodide as iodination agent and the trifluoromethylation system (trifluoromethyl)trimethylsilane/potassium fluoride/copper iodide. This concept could be expanded to perfluoroethylation as well as ethoxycarbonyldifluoromethylation reactions. Copyright

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.