IMPROVED PROCESS FOR THE PREPARATION OF TREPROSTINIL AND DERIVATIVES THEREOF

A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the re...

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Hauptverfasser: NARESHKUMAR F. JAIN, SANJEEVANI A. GHONE, MICHAEL P. KIRKUP, MICHAEL A. MARELLA
Format: Patent
Sprache:eng ; por
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Zusammenfassung:A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.