WO2011110198A8 - A process for making voriconazole - Google Patents

A process for making voriconazole Download PDF

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Publication number
WO2011110198A8
WO2011110198A8 PCT/EP2010/001607 EP2010001607W WO2011110198A8 WO 2011110198 A8 WO2011110198 A8 WO 2011110198A8 EP 2010001607 W EP2010001607 W EP 2010001607W WO 2011110198 A8 WO2011110198 A8 WO 2011110198A8
Authority
WO
WIPO (PCT)
Prior art keywords
making
voriconazole
compound
formula
diastereomers
Prior art date
Application number
PCT/EP2010/001607
Other languages
French (fr)
Other versions
WO2011110198A1 (en
Inventor
Arjanne Overeem
Jie Zhu
Original Assignee
Synthon B.V.
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
Application filed by Synthon B.V. filed Critical Synthon B.V.
Priority to PCT/EP2010/001607 priority Critical patent/WO2011110198A1/en
Priority to EP10708939A priority patent/EP2545039A1/en
Publication of WO2011110198A1 publication Critical patent/WO2011110198A1/en
Publication of WO2011110198A8 publication Critical patent/WO2011110198A8/en

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
    • C07D403/06—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 only aliphatic carbon atoms
    • 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
    • C07D239/30—Halogen atoms or nitro radicals

Abstract

The present invention relates to a process of making a pair of trans-diastereomers of a compound of formula (I) comprising the step of reacting the compound of formula (VI) with an acid or a carboxylate salt thereof of formula (X) wherein M is hydrogen or an equivalent of a metal cation, in the presence of a metal salt in a solvent, and to the use of the compound (X) in making voriconazole.
PCT/EP2010/001607 2010-03-10 2010-03-10 A process for making voriconazole WO2011110198A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/EP2010/001607 WO2011110198A1 (en) 2010-03-10 2010-03-10 A process for making voriconazole
EP10708939A EP2545039A1 (en) 2010-03-10 2010-03-10 A process for making voriconazole

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2010/001607 WO2011110198A1 (en) 2010-03-10 2010-03-10 A process for making voriconazole

Publications (2)

Publication Number Publication Date
WO2011110198A1 WO2011110198A1 (en) 2011-09-15
WO2011110198A8 true WO2011110198A8 (en) 2012-08-16

Family

ID=43127257

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/001607 WO2011110198A1 (en) 2010-03-10 2010-03-10 A process for making voriconazole

Country Status (2)

Country Link
EP (1) EP2545039A1 (en)
WO (1) WO2011110198A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6262972B2 (en) * 2013-09-17 2018-01-17 公益財団法人微生物化学研究会 Compound, method for producing the same, and method for producing voriconazole
CN107827876A (en) * 2017-10-27 2018-03-23 江苏理工学院 A kind of preparation method of voriconazole raceme
CN113929660B (en) * 2021-10-18 2022-10-04 深圳市海滨制药有限公司 Ring opening method of ethylene oxide derivative

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8819308D0 (en) 1988-08-13 1988-09-14 Pfizer Ltd Triazole antifungal agents
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
CN1473825A (en) 2002-08-07 2004-02-11 张文祥 Process for preparing voriconazole
CN1488630A (en) 2002-10-08 2004-04-14 张文更 Method for preparing triazole antifungal agent
CN100379733C (en) 2002-10-08 2008-04-09 南京康泽医药科技有限公司 Method for preparing triazole antifungal agent
EP1828170A4 (en) 2004-12-14 2009-11-11 Reddys Lab Ltd Dr Process for preparing voriconazole
CN1810806A (en) 2005-01-28 2006-08-02 江苏豪森药业股份有限公司 Prepn process and intermediate for voriconazole
EP1899327A1 (en) 2005-06-30 2008-03-19 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)
CN1847243A (en) 2005-07-08 2006-10-18 北京博尔达生物技术开发有限公司 Prepn process and prepn of new soluble voriconazole salt
CN1814597A (en) 2005-12-09 2006-08-09 北京丰德医药科技有限公司 New method for preparing voriconazole
EP2024344A2 (en) 2006-02-01 2009-02-18 Medichem, S.A. Process for preparing voriconazole, new polymorphic form of intermediate thereof, and uses thereof
AR061889A1 (en) 2006-07-13 2008-10-01 Medichem Sa IMPROVED PROCESS FOR THE PREPARATION OF VORICONAZOL
CN1919846B (en) 2006-09-14 2013-01-02 大道隆达（北京）医药科技发展有限公司 Novel oriented synthesis method of voriconazole, medicinal salt and intermediate thereof
CN100478341C (en) 2006-12-31 2009-04-15 中国医学科学院医药生物技术研究所 Voriconazole derivate and preparation process thereof
KR100889937B1 (en) 2007-08-06 2009-03-20 한미약품 주식회사 Process for preparing 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
WO2011110198A1 (en) 2011-09-15
EP2545039A1 (en) 2013-01-16

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