A process for the prepn. of bosentan comprises reaction of chloropyrimidines [I; Z = (protected) OH] with 4-tert-butylbenzenesulfonamide in the presence of base followed by optional deprotection and salification. Thus, I (Z = OH), 4-tert-butylbenzenesulfonamide, CuI, glycine, and K3PO4 were heated together in dioxane at 120° for 44 h to give 31% bosentan.
Taddei, M., Naldini, D., Allegrini, P., Razzetti, G., Mantegazza, S. (2009)Process for the preparation of bosentan via reaction of (protected) 2-[5-(2-methoxyphenoxy)-6-chloro-2-(pyrimidin-2-yl)pyrimidin-4-yloxy]ethanol with 4-tert-butylbenzenesulfonamide. . Brevetto No. US 2009156811 A1 20090618..
Process for the preparation of bosentan via reaction of (protected) 2-[5-(2-methoxyphenoxy)-6-chloro-2-(pyrimidin-2-yl)pyrimidin-4-yloxy]ethanol with 4-tert-butylbenzenesulfonamide
TADDEI, MAURIZIO;
2009-01-01
Abstract
A process for the prepn. of bosentan comprises reaction of chloropyrimidines [I; Z = (protected) OH] with 4-tert-butylbenzenesulfonamide in the presence of base followed by optional deprotection and salification. Thus, I (Z = OH), 4-tert-butylbenzenesulfonamide, CuI, glycine, and K3PO4 were heated together in dioxane at 120° for 44 h to give 31% bosentan.
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https://hdl.handle.net/11365/33887
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