Industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt

Industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt

The present invention relates to an industrial process for the preparation of (5S,10S)-10- benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I) : wherein X is fumarate. This process comprises the following succes...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Lefebvre, Loïc, De Rosa, Sabrina, Poras, Hervé, Gamberoni, Luca, Velardi, Rosario, Zhao, Xinjun
Format: Patent
Sprache:eng
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention relates to an industrial process for the preparation of (5S,10S)-10- benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I) : wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).