METHOD FOR PREPARING DIHYDROQUINOLINONE COMPOUND

To provide methods for preparing 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on.SOLUTION: Methods for preparing crystals of 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dih...

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Hauptverfasser: OKAMURA FUMIYA, KEMMOCHI SUGURU, ANNAKA KIMIYOSHI, MITANI HIKARI, OTSUKA REI, FUJII TAKUYA
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creator OKAMURA FUMIYA
KEMMOCHI SUGURU
ANNAKA KIMIYOSHI
MITANI HIKARI
OTSUKA REI
FUJII TAKUYA
description To provide methods for preparing 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on.SOLUTION: Methods for preparing crystals of 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on are provided which includes the steps of: (1) recycling 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on in a solvent acceptable for preparing pharmaceutical preparations; and (2) cooling and then stirring a solution obtained through the recycling step (1) to obtain the crystal.SELECTED DRAWING: None 【課題】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの製造方法の提供。【解決手段】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの結晶の製造方法であって、(1)5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンを医薬品製造に許容される溶媒中で還流する工程、及び(2)前記還流工程(1)で得られた溶液を冷却して撹拌することにより前記結晶を得る工程を含む方法が提供される。【選択図】なし
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and (2) cooling and then stirring a solution obtained through the recycling step (1) to obtain the crystal.SELECTED DRAWING: None 【課題】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの製造方法の提供。【解決手段】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの結晶の製造方法であって、(1)5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンを医薬品製造に許容される溶媒中で還流する工程、及び(2)前記還流工程(1)で得られた溶液を冷却して撹拌することにより前記結晶を得る工程を含む方法が提供される。【選択図】なし</description><language>eng ; jpn</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>2021</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&amp;date=20211118&amp;DB=EPODOC&amp;CC=JP&amp;NR=2021178818A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,781,886,25569,76552</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20211118&amp;DB=EPODOC&amp;CC=JP&amp;NR=2021178818A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>OKAMURA FUMIYA</creatorcontrib><creatorcontrib>KEMMOCHI SUGURU</creatorcontrib><creatorcontrib>ANNAKA KIMIYOSHI</creatorcontrib><creatorcontrib>MITANI HIKARI</creatorcontrib><creatorcontrib>OTSUKA REI</creatorcontrib><creatorcontrib>FUJII TAKUYA</creatorcontrib><title>METHOD FOR PREPARING DIHYDROQUINOLINONE COMPOUND</title><description>To provide methods for preparing 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on.SOLUTION: Methods for preparing crystals of 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on are provided which includes the steps of: (1) recycling 5-{[(3R, 4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxypiperidine-4-yl] methoxy}-8-fluoro-3,4-dihydroquinoline-2(1H)-on in a solvent acceptable for preparing pharmaceutical preparations; and (2) cooling and then stirring a solution obtained through the recycling step (1) to obtain the crystal.SELECTED DRAWING: None 【課題】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの製造方法の提供。【解決手段】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの結晶の製造方法であって、(1)5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンを医薬品製造に許容される溶媒中で還流する工程、及び(2)前記還流工程(1)で得られた溶液を冷却して撹拌することにより前記結晶を得る工程を含む方法が提供される。【選択図】なし</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>2021</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDDwdQ3x8HdRcPMPUggIcg1wDPL0c1dw8fSIdAnyDwz19PP3AWI_VwVnf98A_1A_Fx4G1rTEnOJUXijNzaDk5hri7KGbWpAfn1pckJicmpdaEu8VYGRgZGhobmFhaOFoTJQiAKV9JzA</recordid><startdate>20211118</startdate><enddate>20211118</enddate><creator>OKAMURA FUMIYA</creator><creator>KEMMOCHI SUGURU</creator><creator>ANNAKA KIMIYOSHI</creator><creator>MITANI HIKARI</creator><creator>OTSUKA REI</creator><creator>FUJII TAKUYA</creator><scope>EVB</scope></search><sort><creationdate>20211118</creationdate><title>METHOD FOR PREPARING DIHYDROQUINOLINONE COMPOUND</title><author>OKAMURA FUMIYA ; 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and (2) cooling and then stirring a solution obtained through the recycling step (1) to obtain the crystal.SELECTED DRAWING: None 【課題】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの製造方法の提供。【解決手段】5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンの結晶の製造方法であって、(1)5−{[(3R,4R)−1−(4−クロロ−2,6−ジフルオロフェニル)−3,4−ジヒドロキシピペリジン−4−イル]メトキシ}−8−フルオロ−3,4−ジヒドロキノリン−2(1H)−オンを医薬品製造に許容される溶媒中で還流する工程、及び(2)前記還流工程(1)で得られた溶液を冷却して撹拌することにより前記結晶を得る工程を含む方法が提供される。【選択図】なし</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 METHOD FOR PREPARING DIHYDROQUINOLINONE COMPOUND
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