PE20130043A1 - Proceso para preparar voriconazol utilizando nuevos intermediarios - Google Patents

Proceso para preparar voriconazol utilizando nuevos intermediarios

Info

Publication number
PE20130043A1
PE20130043A1 PE2012001163A PE2012001163A PE20130043A1 PE 20130043 A1 PE20130043 A1 PE 20130043A1 PE 2012001163 A PE2012001163 A PE 2012001163A PE 2012001163 A PE2012001163 A PE 2012001163A PE 20130043 A1 PE20130043 A1 PE 20130043A1
Authority
PE
Peru
Prior art keywords
formula
compound
iii
voriconazole
substituted
Prior art date
Application number
PE2012001163A
Other languages
English (en)
Inventor
Hyuk Chul Kwon
Man Dong Rho
Kyung Hoi Cha
Original Assignee
Dong Kook Pharm Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42645839&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130043(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Dong Kook Pharm Co Ltd filed Critical Dong Kook Pharm Co Ltd
Publication of PE20130043A1 publication Critical patent/PE20130043A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings

Landscapes

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

Abstract

SE REFIERE A UN PROCESO PARA PREPARAR VORICONAZOL DE FORMULA (I) QUE COMPRENDE: 1) UNA REACCION DE ACOPLAMIENTO DEL TIPO REFORMATSKY ENTRE UN COMPUESTO DERIVADO DE CETONA DE FORMULA (IV) Y UN COMPUESTO DERIVADO DE PIRIMIDINA DE FORMULA (V) PARA OBTENER UN COMPUESTO DE FORMULA (III), A UNA TEMPERATURA ENTRE -15 ºC A 0 ºC; 2) RETIRAR LOS SUSTITUYENTES X1, X2 Y OSO2R DEL COMPUESTO DE FORMULA (III) PARA OBTENER VORICONAZOL RACEMICO DE FORMULA (II), A CONDICION DE QUE NO SE ELIMINEN X1 NI X2 CUANDO AMBOS SON H; USANDO Pd/C, NIQUEL RANEY O ZINC COMO CATALIZADOR, CON UNA CANTIDAD DE Pd/C DE 2 A 30 % EN PESO CON BASE EN LA CANTIDAD DEL COMPUESTO DE FORMULA (III); COMO SOLVENTE, TOLUENO, BENCENO, XILENO O UNA MEZCLA DE ELLOS, Y COMO DONADOR DE HIDROGENO, FORMIATO DE AMONIO O H; Y 3) SEPARAR LOS ISOMEROS DEL COMPUESTO DE FORMULA (II) CON UN ACIDO OPTICAMENTE ACTIVO; X1 Y X2 SON INDEPENDIENTEMENTE H O HALOGENO, R ES ALQUILO C1-4 O FENILO NO SUSTITUIDO O SUSTITUIDO POR NITRO, OXO ENTRE OTROS
PE2012001163A 2010-02-04 2011-02-01 Proceso para preparar voriconazol utilizando nuevos intermediarios PE20130043A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1020100010467A KR100971371B1 (ko) 2010-02-04 2010-02-04 신규한 중간체를 이용한 보리코나졸의 제조방법

Publications (1)

Publication Number Publication Date
PE20130043A1 true PE20130043A1 (es) 2013-02-04

Family

ID=42645839

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012001163A PE20130043A1 (es) 2010-02-04 2011-02-01 Proceso para preparar voriconazol utilizando nuevos intermediarios

Country Status (9)

Country Link
US (1) US8575344B2 (es)
EP (1) EP2531499B1 (es)
JP (1) JP5553911B2 (es)
KR (1) KR100971371B1 (es)
BR (1) BR112012019620A2 (es)
ES (1) ES2518892T3 (es)
MX (1) MX2012008152A (es)
PE (1) PE20130043A1 (es)
WO (1) WO2011096697A2 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101435741B1 (ko) * 2013-01-17 2014-08-29 (주) 에프엔지리서치 신규한 보리코나졸 중간체 및 이를 이용한 보리코나졸의 제조 방법
KR101709543B1 (ko) * 2014-12-09 2017-02-23 (주) 에프엔지리서치 신규한 보리코나졸 중간체 및 이를 이용한 보리코나졸의 제조 방법
CN114829354A (zh) * 2019-12-24 2022-07-29 刘杰 一种伏立康唑对映异构体的回收方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3262386D1 (en) 1981-06-06 1985-03-28 Pfizer Ltd Antifungal agents, processes for their preparation, and pharmaceutical compositions containing them
GB9002375D0 (en) 1990-02-02 1990-04-04 Pfizer Ltd Triazole antifungal agents
GB9516121D0 (en) 1995-08-05 1995-10-04 Pfizer Ltd Organometallic addition to ketones
WO2007013096A1 (en) 2005-06-30 2007-02-01 Msn Laboratories Limited Improved process for the preparation of 2r, 3s-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl) butan-2-ol (voriconazole)
US8143397B2 (en) * 2006-02-01 2012-03-27 Medichem S.A. Process for preparing voriconazole, new polymorphic form of intermediate thereof, and uses thereof
KR100889937B1 (ko) * 2007-08-06 2009-03-20 한미약품 주식회사 보리코나졸의 제조방법
GB2452049A (en) 2007-08-21 2009-02-25 Alpharma Aps Process for the preparation of voriconazole
WO2009084029A2 (en) 2007-12-03 2009-07-09 Neuland Laboratories Ltd Improved process for the preparation of (2r,3s)-2-(2,4- difluqrophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl) butan-2-ol

Also Published As

Publication number Publication date
EP2531499A4 (en) 2013-06-26
EP2531499A2 (en) 2012-12-12
ES2518892T3 (es) 2014-11-05
US8575344B2 (en) 2013-11-05
US20130005973A1 (en) 2013-01-03
KR100971371B1 (ko) 2010-07-20
MX2012008152A (es) 2012-08-23
JP2013518876A (ja) 2013-05-23
BR112012019620A2 (pt) 2022-05-10
EP2531499B1 (en) 2014-07-23
WO2011096697A3 (en) 2011-12-15
WO2011096697A2 (en) 2011-08-11
JP5553911B2 (ja) 2014-07-23

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