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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Hauptverfasser: Lászlófi, István, Rozsumberszki, Imre, Altsach, Tamás, Nagyné Borkó, Ágnes, Havasi, Gábor, Juhász, Imre, Buzder-Lantos, Péter, Hortobágyi, Irén, Kardos, Zsuzsanna
Format: Patent
Sprache:eng
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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.