Process for preparing bosentan
AssigneeGenerics [UK] Limited
InventorsAbhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Vikas Padalkar, Hemant Mande
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Abstract
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.
Claims18
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).
A compound having the structure as shown in formula (2a) or a salt or crystalline form thereof:
- wherein R is a hydroxyl protecting moiety.
A process for preparing a compound of formula (2a) comprising coupling a dichloro compound of formula (1) to a mono-protected ethylene glycol of formula HOCH2CH2OR, wherein R is a hydroxyl protecting moiety, to afford a compound of formula (2a):
Dependencies are inferred from the claim text.