PROCESS FOR THE PREPARATION OF TREPROSTINIL

PROCESS FOR THE PREPARATION OF TREPROSTINIL

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous for...

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Bibliographische Detailangaben
Hauptverfasser: KARDOS, ZSUZSANNA, ALTSACH, TAMÁS, BUZDER-LANTOS, PÉTER, ROZSUMBERSZKI, IMRE, HORTOBÁGYI, IRÉN, LÁSZLÓFI, ISTVÁN, NAGYNÉ BORKÓ, ÁGNES, JUHÁSZ, IMRE, HAVASI, GÁBOR
Format: Patent
Sprache:eng
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.