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

…, LC Campeau, G Hughes, PD O'Shea…

文献索引：Ouellet, Stephane G.; Gauvreau, Danny; Cameron, Mark; Dolman, Sarah; Campeau, Louis-Charles; Hughes, Gregory; O'Shea, Paul D.; Davies, Ian W. Organic Process Research and Development, 2012 , vol. 16, # 2 p. 214 - 219

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被引用次数: 10

摘要

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 ...