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
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creator TANAKA MARIKO
YAMADA KAORU
FUCHIGAMI TAKAMASA
TOIDA NOBUKO
description 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.
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subjects 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
title 1,3-DISUBSTITUTED-5-FLUORO-6-IODOURACIL DERIVATIVE AND ANTITUMOR AGENT
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