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...

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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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creator	ANGEL NIKOLOV KONAKCHIEV ILIYA VASSILEV OGNYANOV RALPH HANNI
description	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.
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title	Process for the preparation of dihydroartemisinin hemisucinate
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