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US 2014/0275535 A1Published application
Acid addition salts of bosentan
AssigneeBiocon Limited
InventorsSrinivas Pullela Venkata, Kiran Kumar Kothakonda, Shanmughasamy Rajmahendra, Indrajit Chandrasekaran, Mariappan Kaliappan, Rekha Shivappa Mailar
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Abstract
The present invention relates to the stable acid addition salts of Bosentan that are useful for the purification of Bosentan base. In particular, the Bosentan acid addition salt is selected from Bosentan citrate and Bosentan tartrate.
Claims19
Acid addition salts of Bosentan.
A method of making an acid addition salt of Bosentan, which comprises:
- a) combining Bosentan base and an acid having a pKa higher than 3 in an organic solvent to form a solution;
- b) precipitating a Bosentan acid addition salt from said solution and c) isolating the precipitated Bosentan acid addition salt.
A method of purifying Bosentan, which comprises:
- a) preparation of an acid addition salt of Bosentan by following any method discussed in earlier claims, b) isolation of said acid addition salt of Bosentan from organic solvent c) optionally re crystallizing by using an organic solvent d) converting Bosentan acid addition salt into Bosentan base and e) isolation of Bosentan base.
Bosentan citrate salt.
Bosentan tartarate salt.
Dependencies are inferred from the claim text.