Treprostinyl-sodium-monohydrate and process for its preparation

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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Main Authors Rozsumberszki Imre, Nagyne Borko Agnes, Buzder-Lantos Peter, Juhasz Imre, Kardos Zsuzsanna, Altsach Tamas, Havasi Gabor, Laszlofi Istvan, Hortobagyi Iren
Format Patent
LanguageEnglish
Hungarian
Published 28.07.2021
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Summary: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.
Bibliography:Application Number: HUP1900346