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US 12,435,042 B2Granted
Process for the preparation of key intermediates for the synthesis of Eltrombopag or salt thereof
AssigneeF.I.S. Fabbrica Italiana Sintetici S.p.A.
InventorsPaolo Stabile, Floriana Semeraro
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Abstract
Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.
Claims4
A process for the preparation of Eltrombopag of formula (I) or salt thereof:
- comprising of the following steps:
- A) Palladium catalyzed coupling of 3-carboxyphenylboronic acid of formula (II):
- with the potassium salt of 2-bromo-4-chlorophenol of formula (III):
- to obtain the compound of formula (IV) or a hydrate thereof:
- wherein A is potassium;
- B) nitration of the compound of formula (IV) prepared in the step A) in presence of acetic acid and 65% nitric acid to the compound of formula (V):
- C) hydrogenation of compound of formula (V) obtained in the step B) to compound of formula (VI) or its hydrate form:
- D) conversion of compound of formula (VI) obtained in the step C) to Eltrombopag of formula (I) or salt thereof.
5 more elements
Dependencies are inferred from the claim text.