DK2612859T3 - Fremgangsmåde til fremstilling af 1-triazol-2-butanol-derivat. - Google Patents

Fremgangsmåde til fremstilling af 1-triazol-2-butanol-derivat. Download PDF

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Publication number
DK2612859T3
DK2612859T3 DK11821851.0T DK11821851T DK2612859T3 DK 2612859 T3 DK2612859 T3 DK 2612859T3 DK 11821851 T DK11821851 T DK 11821851T DK 2612859 T3 DK2612859 T3 DK 2612859T3
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Denmark
Prior art keywords
acid
methylenepiperidine
reaction
addition salt
production
Prior art date
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DK11821851.0T
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English (en)
Inventor
Mitsuo Mimura
Masahito Watanabe
Nobuo Ishiyama
Takuya Yamada
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Kaken Pharma Co Ltd
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Publication of DK2612859T3 publication Critical patent/DK2612859T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (6)

1. Fremgangsmåde til fremstilling af (2R,3R)-2-(2,4-difluorphenyl)-3-(4-methylenpiperidin-l-yl)-l-(l/-/-l,2,4-triazol-l-yl)butan-2-ol eller et syreadditionssalt deraf, som omfatter at reagere (2R,3S)-2-(2,4-difluorphenyl)-3-methyl-2-[(l/-/-l,2,4-triazol-l-yl)methyl]oxiran med et syreadditionssalt af 4-methylenpiperidin i et reaktionssolvent under tilstedeværelse af en hydroxid af et alkalimetal eller et alkalijordmetal valgt fra gruppen bestående af lithium og calcium, eller et hydrat deraf.
2. Fremgangsmåde ifølge krav 1, hvor hydroxiden af et alkalimetal eller et alkalijordmetal er lithiumhydroxid.
3. Fremgangsmåde ifølge krav 1 eller 2, hvor syreadditionssaltet af 4-methylenpiperidin er 4-methylenpiperidinhydrobromid eller 4-methylenpiperidinhydroiodid.
4. Fremgangsmåde ifølge krav 3, hvor syreadditionssaltet af 4-methylenpiperidin er 4-methylenpiperidinhydrobromid.
5. Fremgangsmåde ifølge et hvilket som helst af krav 1 til 4, hvor reaktionssolventet er acetonitril, 1,2-dimethoxyethan, cyclopentylmethylether, isopropanol, 1-butanol, eller 4-methyl-2-pentanon.
6. Fremgangsmåde ifølge krav 5, hvor reaktionssolventet er acetonitril eller cyclopentylmethylether.
DK11821851.0T 2010-08-31 2011-08-31 Fremgangsmåde til fremstilling af 1-triazol-2-butanol-derivat. DK2612859T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2010194068 2010-08-31
PCT/JP2011/069733 WO2012029836A1 (ja) 2010-08-31 2011-08-31 1-トリアゾール-2-ブタノール誘導体の製造法

Publications (1)

Publication Number Publication Date
DK2612859T3 true DK2612859T3 (da) 2015-10-19

Family

ID=45772914

Family Applications (1)

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DK11821851.0T DK2612859T3 (da) 2010-08-31 2011-08-31 Fremgangsmåde til fremstilling af 1-triazol-2-butanol-derivat.

Country Status (15)

Country Link
US (1) US8871942B2 (da)
EP (2) EP2966071B1 (da)
JP (1) JP5852573B2 (da)
CN (2) CN106045970B (da)
BR (1) BR112013004827B1 (da)
CA (1) CA2808230C (da)
CY (1) CY1116997T1 (da)
DK (1) DK2612859T3 (da)
ES (1) ES2556782T3 (da)
HU (1) HUE026357T2 (da)
PL (1) PL2612859T3 (da)
PT (1) PT2612859E (da)
RS (1) RS54330B1 (da)
TW (1) TWI518081B (da)
WO (1) WO2012029836A1 (da)

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Publication number Priority date Publication date Assignee Title
US20090175810A1 (en) 2008-01-03 2009-07-09 Gareth Winckle Compositions and methods for treating diseases of the nail
US8039494B1 (en) 2010-07-08 2011-10-18 Dow Pharmaceutical Sciences, Inc. Compositions and methods for treating diseases of the nail
AU2014329421B2 (en) 2013-10-03 2018-08-02 Dow Pharmaceutical Sciences, Inc. Stabilized efinaconazole compositions
WO2015077729A2 (en) 2013-11-22 2015-05-28 Dow Pharmaceutical Sciences, Inc. Anti-infective methods, compositions, and devices
CN104292214B (zh) * 2014-09-24 2017-04-05 南京华威医药科技开发有限公司 艾氟康唑及其中间体的合成方法
CN104327047B (zh) * 2014-10-17 2016-04-06 苏州明锐医药科技有限公司 艾菲康唑的制备方法
CA2910990C (en) * 2014-11-23 2022-03-22 Mapi Pharma Ltd. Intermediate compounds and process for the preparation of efinaconazole
CA2974180A1 (en) * 2015-01-20 2016-07-28 Itai Adin Crystalline forms of efinaconazole
ITUB20150417A1 (it) * 2015-05-08 2016-11-08 Dipharma Francis Srl Procedimento per la preparazione di composti piperidinici
US10479776B2 (en) 2015-05-12 2019-11-19 Lupin Limited Process for the preparation of Efinaconazole
US10125115B2 (en) 2015-06-04 2018-11-13 Glenmark Pharmaceuticals Limited Process for the preparation of efinaconazole
EP3112360A1 (en) 2015-06-29 2017-01-04 Dipharma Francis S.r.l. Process for the preparation of efinaconazole
CN106565672A (zh) * 2015-10-08 2017-04-19 中美华世通生物医药科技(武汉)有限公司 制备艾氟康唑的方法
US20170129874A1 (en) * 2015-11-10 2017-05-11 Virupaksha Organics Limited Novel improved process for preparing a triazole antifungal agent
CN106810534A (zh) * 2015-11-30 2017-06-09 中美华世通生物医药科技(武汉)有限公司 艾氟康唑晶型及其制备方法
CN106918672B (zh) * 2015-12-28 2021-02-09 中美华世通生物医药科技(武汉)有限公司 利用hplc测定艾氟康唑原料药及其制剂中有关物质的方法
CN106928186A (zh) * 2015-12-29 2017-07-07 中美华世通生物医药科技(武汉)有限公司 化合物及其制备方法和用途
ITUB20159795A1 (it) * 2015-12-30 2017-06-30 Procos Spa Processo per la sintesi di efinaconazolo
CN106995434A (zh) * 2016-01-25 2017-08-01 广东东阳光药业有限公司 一种***类抗真菌药的晶型及其制备方法
ITUA20162545A1 (it) * 2016-04-13 2017-10-13 Laboratorio Chimico Int S P A Procedimento per la preparazione di intermedi utili nella sintesi di farmaci
CN107759565B (zh) * 2016-08-15 2020-10-23 苏州旺山旺水生物医药有限公司 一种1-***-2-丁醇衍生物的制备方法
CN107778283A (zh) * 2016-08-26 2018-03-09 山东特珐曼药业有限公司 一种艾氟康唑的制备方法和其晶型m
WO2018036416A1 (zh) * 2016-08-26 2018-03-01 山东特珐曼药业有限公司 一种艾氟康唑的制备方法和其晶型m
CN108276381A (zh) * 2017-01-06 2018-07-13 上海和博药物研究有限公司 一种艾氟康唑的合成方法
IT201700048270A1 (it) * 2017-05-04 2018-11-04 Seegpharm Sa Procedimento per la preparazione di un derivato azolico.
ES2941251T3 (es) 2017-05-19 2023-05-19 Kaken Pharma Co Ltd Métodos de producción y purificación de efinaconazol
CN108440390A (zh) * 2018-03-13 2018-08-24 上药康丽(常州)药业有限公司 一种4-亚甲基哌啶盐的制备方法
WO2020133411A1 (zh) 2018-12-29 2020-07-02 山东威智医药工业有限公司 一种艾氟康唑的制备方法
CN113929660B (zh) * 2021-10-18 2022-10-04 深圳市海滨制药有限公司 一种环氧乙烷衍生物开环方法

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JPH02191262A (ja) 1988-03-04 1990-07-27 Sankyo Co Ltd トリアゾール誘導体
ES2110749T3 (es) * 1993-05-10 1998-02-16 Kaken Pharma Co Ltd Derivado de azolilamina.
CN1125814C (zh) * 1995-09-28 2003-10-29 科研制药株式会社 4-亚甲基哌啶的制备方法

Also Published As

Publication number Publication date
ES2556782T3 (es) 2016-01-20
CN106045970A (zh) 2016-10-26
BR112013004827B1 (pt) 2020-03-31
TW201215601A (en) 2012-04-16
EP2966071B1 (en) 2017-01-25
EP2966071A1 (en) 2016-01-13
PT2612859E (pt) 2015-11-30
PL2612859T3 (pl) 2016-01-29
US20130150586A1 (en) 2013-06-13
EP2612859B1 (en) 2015-09-30
JPWO2012029836A1 (ja) 2013-10-31
HUE026357T2 (en) 2016-06-28
US8871942B2 (en) 2014-10-28
BR112013004827A2 (pt) 2016-05-31
CN103080100B (zh) 2016-04-27
RS54330B1 (en) 2016-02-29
CN103080100A (zh) 2013-05-01
CA2808230C (en) 2017-02-28
JP5852573B2 (ja) 2016-02-03
EP2612859A4 (en) 2014-01-08
CN106045970B (zh) 2019-11-08
EP2612859A1 (en) 2013-07-10
CA2808230A1 (en) 2012-03-08
WO2012029836A1 (ja) 2012-03-08
CY1116997T1 (el) 2017-04-05
TWI518081B (zh) 2016-01-21

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