(E)-5-(2-BROMOVINYL)-URIDINE, ITS DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

(E)-5-(2-BROMOVINYL)-URIDINE, ITS DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

The invention relates to (E)-5-(2-bromovinyl)-uridine and its derivatives of general formula VI, VI wherein R1 stands for a hydrogen atom, C1-8 alkanoyl group, benzoyl group or a benzoyl group substituted in para position either with a C1-4 alkyl group or a halogen atom, and a process for preparing...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: ILDIKO FRITZSCHE, ISTVAN HORVATH, PAL IVAN, ANNA SZABOLCS, JANOS SAGI, JANOS NAGY, LASZLO OTVOS, MARIA PEREDY, ISTVAN KOCZKA, CSILLA RETHATI, ATTILA SZEMZO
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
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Beschreibung
Zusammenfassung:The invention relates to (E)-5-(2-bromovinyl)-uridine and its derivatives of general formula VI, VI wherein R1 stands for a hydrogen atom, C1-8 alkanoyl group, benzoyl group or a benzoyl group substituted in para position either with a C1-4 alkyl group or a halogen atom, and a process for preparing them by brominating 2',3',5'-tri-O-acyl-5-ethyl-uridine of general formula IV, IV wherein R is identical with R1, except where R1 stands for a hydrogen atom, dehydrohalogenating the resulting dibromo compound of general formula V V and optionally deacylating it. The resulting compounds of general formula VI are exhibiting significant potency against Herpes simplex virus species and are of remarkably low acute toxicity.