CYTIDINE DERIVATIVE

NEW MATERIAL:The compound of formula I (X is halogen) and its salt. EXAMPLE:3'-Deoxy-3'-iodocytidine. USE:Carcinostatic agent. PREPARATION:The objective compound can be produced e.g. by (1) reacting the compound of formula II (R1 is lower acyl) (e.g. N-acetyl-cytosine) with a trimethylsily...

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Bibliographische Detailangaben
Hauptverfasser:	YAMAMOTO MANAI, MATSUMOTO KENSUKE, HOSOGAMI TOORU
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:	NEW MATERIAL:The compound of formula I (X is halogen) and its salt. EXAMPLE:3'-Deoxy-3'-iodocytidine. USE:Carcinostatic agent. PREPARATION:The objective compound can be produced e.g. by (1) reacting the compound of formula II (R1 is lower acyl) (e.g. N-acetyl-cytosine) with a trimethylsilylation agent (e.g. hexamethyldisilazane) in a solvent such as dichloromethane under heating, (2) removing unreacted trimethylsilylation agent by e.g. distillation, (3) reacting the reaction product with the compound of formula III (R2 is lower acyl; R3 is 4-nitrobenzoyl, etc.) [e.g. 1,2-di-O-acetyl-3-deoxy-3- iodo-5-O-(p-nitrobenzoyl)-beta-D-ribofuranose] in the presence of a Lewis acid such as tin tetrachloride without separating the reaction product from the system and (4) deacylating the resultant compound of formula IV.