1044277-07-7

Upstream product

• 1044277-06-6 4-(3-fluorophenyl)-7-methyl-2H-chromen-2-one 
• 167840-97-3 7-Methylcoumarin-4-yl trifluoromethanesulfonate 
• 6921-64-8 4'-hydroxy-2'-methylacetophenone 
• 122-46-3 3-acetoxytoluene 
• 455-38-9 3-fluorobenzoic acid 
• 33166-77-7 ethyl 3-(3-fluorophenyl)-3-oxopropanoate 
• 108-39-4 3-methyl-phenol 

Downstream Products

• 1044277-08-8 7-(azidomethyl)-4-(3-fluorophenyl)-2H-chromen-2-one 
• 1044277-09-9 (1S)-1-(1-{[4-(3-fluorophenyl)-2-oxo-2H-chromen-7-yl]-methyl}-1H-1,2,3-triazol-4-yl)-1-(trifluoromethyl)propyl 4-nitrobenzoate 
• 1044277-01-1 (1S)-1-(1-{[4-(3-fluorophenyl)-2-oxo-2H-chromen-7-yl]-methyl}-1H-1,2,3-triazol-4-yl)-1-(trifluoromethyl)propyl 4-nitrobenzoate 

Relevant academic research and scientific papers

Convergent, fit-for-purpose, kilogram-scale synthesis of a 5-lipoxygenase inhibitor

Process research and development of a synthetic route towards a novel 5-lipoxygenase inhibitor is described. The synthetic route provided 1 in 27% yield in nine steps (seven steps in the longest linear sequence) and was performed on kilogram scale. The synthesis began with the preparation of the coumarin core via an efficient von Pechmann condensation. The triazole fragment was obtained via a regioselective copper-catalyzed [3 + 2] cycloaddition between a chiral alkyne and the coumarin azide.

Novel pharmaceutical compounds

The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.