PROCESS FOR PRODUCING N-DESMETHYLVINBLASTINE, VINCRISTINE, N-DESMETHYLLEUROSINE, H-DIMETHYL-N-FORMYLLEUROSINE, N-DISMETHYL-N-(ETHOXYMETHYL)-VINBLASTINE, N-DESMETHYL-N-(ETHOXYMETHYL)-LEUROSINE OR THEIR SALTS

PROCESS FOR PRODUCING N-DESMETHYLVINBLASTINE, VINCRISTINE, N-DESMETHYLLEUROSINE, H-DIMETHYL-N-FORMYLLEUROSINE, N-DISMETHYL-N-(ETHOXYMETHYL)-VINBLASTINE, N-DESMETHYL-N-(ETHOXYMETHYL)-LEUROSINE OR THEIR SALTS

A proces for the oxidation of vinblastine, leurosine or an acid addition salt thereof which comprises reacting the vinblastine, leurosine or acid addition salt thereof with chromic acid or an alkali metal dichromate, at a temperature of from -30 °C to 90°C in the presence of a water immiscible organ...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: YANOSH SHUGAR,HU, KAROLA JOVANOVICH,HU, SHANDOR GEGEG,HU, ELEK FARKASH,HU, SHANDOR EKKHARDT,HU, ZHUZHA SHOMFAI,HU, IVAN KHINDI,HU
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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Beschreibung
Zusammenfassung:A proces for the oxidation of vinblastine, leurosine or an acid addition salt thereof which comprises reacting the vinblastine, leurosine or acid addition salt thereof with chromic acid or an alkali metal dichromate, at a temperature of from -30 °C to 90°C in the presence of a water immiscible organic solvent in which alkaloids are readily soluble, acetic anhydride and optionally glacial acetic acid and/or up to 10% by volume of ethanol based on the volume of the water-immiscible organic solvent; thereafter adjusting the pH of the reaction mixture to from 8 to 10; and isolating the products obtained and/or subjecting the said products to further treatment.The specification also describes new bis-indole-alkaloids, pharmaceutical compositions containing them and their use as anti-tumour agents.