95392-17-9

Upstream product

• 456-48-4 3-Fluorobenzaldehyde 
• 95392-11-3 Fluoro-(3-fluoro-phenyl)-acetonitrile 
• 1208004-83-4 1-(2-azido-1-fluoroethyl)-3-fluorobenzene 
• 100948-28-5 2-(3-fluorophenyl)-2-((trimethylsilyl)oxy)acetonitrile 

Downstream Products

• 1329998-89-1 C₃₆H₅₂F₂N₄O₇ 

Relevant academic research and scientific papers

Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability

Recently, a series of potent and selective neuronal nitric oxide synthase inhibitors containing two basic nitrogen atoms was reported (Ji, H.; Stanton, B. Z.; Igarashi, J.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Am. Chem. Soc. 2008, 130, 3900-3914). In an effort to improve their bioavailability, three compounds (2a-c) were designed with electron-withdrawing groups near one of the basic nitrogen atoms to lower its pKa. Inhibition studies with these compounds showed that two of them not only retained most of the potency and selectivity of the best analogue of the earlier series, but also showed improved membrane permeability based on data from a cell-based assay.

POTENT AND SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS WITH IMPROVED MEMBRANE PERMEABILITY

Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.

Synthesis of β-fluorophenethyl halopyridyl thiourea compounds as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Synthesis of β-fluorophenethylamines was accomplished in three steps with an overall yield of 50%. Condensation of β-fluorophenethylamine hydrochloride with thiocarbonylimidazole derivative derived from halopyridyl amines in dimethylformamide furnished the desired thiourea compounds as crystalline solids. Several of the β-fluorophenethyl thiourea compounds inhibited HIV-1 reverse transcriptase (RT) at nanomolar to low micromolar concentrations.

A NOVEL SYNTHESIS OF α-FLUOROOACETONITRILES. APPLICATION TO A CONVENIENT PREPARATION OF 2-FLUORO-2-PHENETYLAMINES

α-Fluorophenylacetonitriles (3) are readily prepared by the treatment of the corresponding benzaldehyde cyanohydrin trimethylsilylethers (2) with diethylaminosulfur trifluoride (DAST).This method for the introduction of fluorine alpha to the cyano group is also applicable to the cyanohydrin trimethylsilylethers of aromatic ketones.Diborane reduction of the α-fluorophenylacetonitriles (3) yields 2-fluoro-2-phenethylamines (4).