1,3-DISUBSTITUTED-5-FLUORO-6-IODOURACIL DERIVATIVE AND ANTITUMOR AGENT

NEW MATERIAL:A 1,3-disubstituted-5-fluoro-6-iodouracil derivative expressed by formula I (R and R are alkyl, alkenyl, aralkyl or oxygen-containing heterocyclic group). EXAMPLE:1,3-Dimethyl-5-fluoro-6-iodouracil. USE:An antitumor agent having improved toxicity of 5-fluorouracil and higher inhibition...

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Hauptverfasser:	TANAKA MARIKO, YAMADA KAORU, FUCHIGAMI TAKAMASA, TOIDA NOBUKO
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:	NEW MATERIAL:A 1,3-disubstituted-5-fluoro-6-iodouracil derivative expressed by formula I (R and R are alkyl, alkenyl, aralkyl or oxygen-containing heterocyclic group). EXAMPLE:1,3-Dimethyl-5-fluoro-6-iodouracil. USE:An antitumor agent having improved toxicity of 5-fluorouracil and higher inhibition ratio of malignant tumor than that of 6-chloro derivatives. PREPARATION:A compound expressed by formula II is reacted in the presence of a base, e.g. butyllithium, lithium diisopropylamide, etc., preferably in an ether based solvent, e.g. diethyl ether, tetrahydrofuran, etc., to give a compound expressed by formula III, which is then reacted with an iodinating agent, e.g. iodine monochloride, iodine, etc., preferably in the above-mentioned solvent to afford the aimed compound expressed by formula I.