379-40-8

Upstream product

• 427-24-7 diphenyl-ortho-fluorophenyl-methanol 
• 75-36-5 acetyl chloride 
• 394-35-4 methyl 2-fluorobenzoate 

Downstream Products

• 23593-78-4 CDD 3524 
• 197526-04-8 2-(2-fluorophenyl)-2,2-diphenylacetonitrile 
• 22763-56-0 2-fluoro-trityl 
• 464-52-8 1,2-bis-(2-fluoro-phenyl)-1,1,2,2-tetraphenyl-ethane 

Relevant academic research and scientific papers

Novel inhibitors of the gardos channel for the treatment of sickle cell disease

Sickle cell disease (SCD) is a hereditary condition characterized by deformation of red blood cells (RBCs). This phenomenon is due to the presence of abnormal hemoglobin that polymerizes upon deoxygenation. This effect is exacerbated when dehydrated RBCs experience a loss of both water and potassium salts. One critical pathway for the regulation of potassium efflux from RBCs is the Gardos channel, a calcium-activated potassium channel. This paper describes the synthesis and biological evaluation of a series of potent inhibitors of the Gardos channel. The goal was to identify compounds that were potent and selective inhibitors of the channel but had improved pharmacokinetic properties compared to 1, Clotrimazole. Several triarylamides such as 10 and 21 were potent inhibitors of the Gardos channel (IC50 of 10 nM) and active in a mouse model of SCD. Compound 21 (ICA-17043) was advanced into phase 3 clinical trials for SCD.

Synthesis and reactivity of cyclopentadienyl and indenyl ligands bearing ω-fluorinated pendant groups. Crystal structure of (ortho-F-C6H4)-CPh2-C5H 4SiMe3

A series of cyclopentadienes and indenes with ω-fluorinated pendant groups have been synthesised and their reactivity towards metallating agents n-BuLi, NaH, TIOEt, Me3SiCl, Me3SnCl, TiHal4, ZrX4 (X = Cl, NMe2) has been investigated. The crystal structure of 1-trimethylsilyl-3-(diphenyl-ortho-fluorophenyl-methyl)-cyclopentadiene (3) was determined.

Synthesis and antifungal activity of a series of difluorotritylimidazoles

1-[(2-Fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole (flutrimazole, UR-4056, CAS 119006-77-8) (15) was selected among a series of mono-, di- and trifluorotrityl-imidazole antifungal agents as the most potent fluorine containing analogue of clotrimazole.