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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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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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.</description><language>eng</language><subject>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</subject><creationdate>1987</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19871006&DB=EPODOC&CC=JP&NR=S62228069A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25555,76308</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19871006&DB=EPODOC&CC=JP&NR=S62228069A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>TANAKA MARIKO</creatorcontrib><creatorcontrib>YAMADA KAORU</creatorcontrib><creatorcontrib>FUCHIGAMI TAKAMASA</creatorcontrib><creatorcontrib>TOIDA NOBUKO</creatorcontrib><title>1,3-DISUBSTITUTED-5-FLUORO-6-IODOURACIL DERIVATIVE AND ANTITUMOR AGENT</title><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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1987</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZHAz1DHWdfEMDnUKDvEMCQ1xddE11XXzCfUP8tc10_X0d_EPDXJ09vRRcHEN8gxzDPEMc1Vw9HMBYpByX_8gBUd3V78QHgbWtMSc4lReKM3NoOjmGuLsoZtakB-fWlyQmJyal1oS7xUQbGZkZGRhYGbpaEyMGgCjWCyO</recordid><startdate>19871006</startdate><enddate>19871006</enddate><creator>TANAKA MARIKO</creator><creator>YAMADA KAORU</creator><creator>FUCHIGAMI TAKAMASA</creator><creator>TOIDA NOBUKO</creator><scope>EVB</scope></search><sort><creationdate>19871006</creationdate><title>1,3-DISUBSTITUTED-5-FLUORO-6-IODOURACIL DERIVATIVE AND ANTITUMOR AGENT</title><author>TANAKA MARIKO ; YAMADA KAORU ; FUCHIGAMI TAKAMASA ; TOIDA NOBUKO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_JPS62228069A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1987</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>TANAKA MARIKO</creatorcontrib><creatorcontrib>YAMADA KAORU</creatorcontrib><creatorcontrib>FUCHIGAMI TAKAMASA</creatorcontrib><creatorcontrib>TOIDA NOBUKO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>TANAKA MARIKO</au><au>YAMADA KAORU</au><au>FUCHIGAMI TAKAMASA</au><au>TOIDA NOBUKO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>1,3-DISUBSTITUTED-5-FLUORO-6-IODOURACIL DERIVATIVE AND ANTITUMOR AGENT</title><date>1987-10-06</date><risdate>1987</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record> |
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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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