Process for the preparation of dihydroartemisinin hemisucinate

Process for the preparation of dihydroartemisinin hemisucinate

Prepn. of the 10 alpha -epimer of dihydroartemisinin hemisuccinate of formula (I) comprises acylation of dihydroartemisinin of formula (II) with succinic anhydride (SA). The acylation is effected using 1.0-1.3 molar equivs. of SA in presence of 0.1-1.5 molar equivs. (based on (II)) of a tri-(1-3C al...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: ANGEL NIKOLOV KONAKCHIEV, ILIYA VASSILEV OGNYANOV, RALPH HANNI
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:Prepn. of the 10 alpha -epimer of dihydroartemisinin hemisuccinate of formula (I) comprises acylation of dihydroartemisinin of formula (II) with succinic anhydride (SA). The acylation is effected using 1.0-1.3 molar equivs. of SA in presence of 0.1-1.5 molar equivs. (based on (II)) of a tri-(1-3C alkyl)amine, in a low-boiling, neutral, water-miscible inert organic solvent (or solvent mixt.). (I) is then isolated at pH 5-8.