CONVERSION OF URACIL DERIVATIVES TO CYTOSINE DERIVATIVES

CONVERSION OF URACIL DERIVATIVES TO CYTOSINE DERIVATIVES

A process is disclosed for producing a 4-O-sulfonyluracil derivative of the formula [wherein R1 is hydrogen, halogen, alkyl and alkoxy, R2 is glycosyl having protected hydroxyls; and -SO2R3 is an organic sulfonyl] which comprises reacting an uracil derivative of the formula [wherein R1 and R2 are as...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: MITSURU KAWADA, KIYOHARU MATSUMOTO, MASAAKI TSURUSHIMA
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Beschreibung
Zusammenfassung:A process is disclosed for producing a 4-O-sulfonyluracil derivative of the formula [wherein R1 is hydrogen, halogen, alkyl and alkoxy, R2 is glycosyl having protected hydroxyls; and -SO2R3 is an organic sulfonyl] which comprises reacting an uracil derivative of the formula [wherein R1 and R2 are as defined above] with an organic sulfonylating agent of the formula R3SO2X [wherein R3SO2 is an organic sulfonyl and X is halogen] in the presence of potassium carbonate. The obtained 4-O-sulfonyluracil is further subjected to amination. The processes are industrially adavantageous and produce cytosine derivatives such as cytidine in high yield.