Process for preparing bosentan

摘要

The present invention relates to a novel intermediate useful in the preparation of bosentan and to processes for the preparation of said intermediate and bosentan. The invention further relates to compositions comprising bosentan prepared according to the processes of the invention and their use in the treatment of endothelin-receptor mediated disorders.

主权项

1. A process for preparing bosentan comprising:
(a) reacting a dichloro compound of formula (1) with a mono-protected ethylene glycol of formula HOCH2CH2OR, wherein R is a hydroxyl protecting moiety, to afford a compound of formula (2a): (b) coupling compound (2a) with 4-tert-butyl phenyl sulfonamide; (c) removing the protecting moiety R; and (d) isolating bosentan from the mixture obtained in step (c).