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US 8,772,503 B2Granted
Processes for the preparation of deferasirox, and deferasirox polymorphs
AssigneeMapi Pharma Ltd.
InventorsMichael Mizhiritskii, Ehud Marom, Shai Rubnov
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Abstract
The present invention relates to processes for the preparation of deferasirox, an oral iron chelator developed to treat iron overload due to e.g. multiple blood transfusions. The present invention further provides novel deferasirox pseudopolymorphs and a novel amorphous form of deferasirox, processes for their preparation, as well as pharmaceutical compositions comprising same, and use thereof in treating iron overload.
Claims10
A process for the preparation of deferasirox, comprising the steps of:
- a) converting salicylic acid to its acyl chloride:
- b) reacting salicyl chloride with an amidating reagent so as to produce a deferasirox intermediate of formula:
- and
- c) reacting intermediate with 4-hydrazinobenzoic acid to form deferasirox:
1 more element
Dependencies are inferred from the claim text.