PRODUCTION OF UCN-01

PRODUCTION OF UCN-01

PURPOSE:To efficiently and simply obtain UCN-01 having antitumor action or antimicrobial action by oxidizing staurosporine in dimethyl sulfoxide and an aqueous solution of an alkali. CONSTITUTION:Staurosporine of formula I is oxidized in a solution comprising dimethyl sulfoxide and an aqueous soluti...

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Bibliographische Detailangaben
Hauptverfasser: MURAGATA TSUTOMU, MIHARA AKIRA, TAKAHASHI KEIICHI, TAKIGUCHI TOSHIMITSU, SAITO HIROMITSU, KATSUMATA SHIGEO
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:PURPOSE:To efficiently and simply obtain UCN-01 having antitumor action or antimicrobial action by oxidizing staurosporine in dimethyl sulfoxide and an aqueous solution of an alkali. CONSTITUTION:Staurosporine of formula I is oxidized in a solution comprising dimethyl sulfoxide and an aqueous solution of an alkali (e.g. NaOH) at 0-50 deg.C for 1-24 hours to give UCN-01 of formula II. The blending ratio of the dimethyl sulfoxide and the aqueous solution of an alkali is preferably 2/1-10/1 and 5-100ml of the mixed solvent is used based on 1g staurosporine. The concentration of the aqueous solution of alkali is preferably 0.1N-10N.