DE69924651D1 - Verfahren zu Herstellung von 1,3-Oxathiolane Nukleosiden - Google Patents

Verfahren zu Herstellung von 1,3-Oxathiolane Nukleosiden

Info

Publication number
DE69924651D1
DE69924651D1 DE69924651T DE69924651T DE69924651D1 DE 69924651 D1 DE69924651 D1 DE 69924651D1 DE 69924651 T DE69924651 T DE 69924651T DE 69924651 T DE69924651 T DE 69924651T DE 69924651 D1 DE69924651 D1 DE 69924651D1
Authority
DE
Germany
Prior art keywords
preparation
oxathiolane
oxathiolane nucleosides
nucleosides
processes
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE69924651T
Other languages
English (en)
Inventor
Darryl Cleary
Jose Soria
George R Painter
Dennis C Liotta
Merrick Almond
Marcos Luis Sznaidman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Emory University
Gilead Sciences Inc
Original Assignee
Emory University
Gilead Sciences Inc
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 Emory University, Gilead Sciences Inc filed Critical Emory University
Application granted granted Critical
Publication of DE69924651D1 publication Critical patent/DE69924651D1/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
    • C07D327/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
DE69924651T 1998-08-12 1999-08-12 Verfahren zu Herstellung von 1,3-Oxathiolane Nukleosiden Expired - Lifetime DE69924651D1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9621498P 1998-08-12 1998-08-12
US12284199P 1999-03-04 1999-03-04

Publications (1)

Publication Number Publication Date
DE69924651D1 true DE69924651D1 (de) 2005-05-12

Family

ID=26791450

Family Applications (2)

Application Number Title Priority Date Filing Date
DE69921829T Expired - Lifetime DE69921829T2 (de) 1998-08-12 1999-08-12 Verfahren zur herstellung von 1,3-oxathiolannukleoside
DE69924651T Expired - Lifetime DE69924651D1 (de) 1998-08-12 1999-08-12 Verfahren zu Herstellung von 1,3-Oxathiolane Nukleosiden

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DE69921829T Expired - Lifetime DE69921829T2 (de) 1998-08-12 1999-08-12 Verfahren zur herstellung von 1,3-oxathiolannukleoside

Country Status (17)

Country Link
US (4) US6215004B1 (de)
EP (4) EP1104415B1 (de)
JP (4) JP4249393B2 (de)
KR (3) KR100856416B1 (de)
CN (1) CN1141305C (de)
AT (2) ATE292631T1 (de)
AU (2) AU771779B2 (de)
BR (1) BR9912951B1 (de)
CA (3) CA2714085C (de)
DE (2) DE69921829T2 (de)
ES (2) ES2537540T3 (de)
HK (2) HK1038921A1 (de)
IL (4) IL141359A0 (de)
MX (1) MXPA01001552A (de)
PT (2) PT2322518E (de)
RU (2) RU2439069C2 (de)
WO (1) WO2000009494A1 (de)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
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US6175008B1 (en) * 1988-04-11 2001-01-16 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
DE69921829T2 (de) * 1998-08-12 2005-10-27 Gilead Sciences, Inc., Foster City Verfahren zur herstellung von 1,3-oxathiolannukleoside
CA2308559C (en) 2000-05-16 2005-07-26 Brantford Chemicals Inc. 1,3-oxathiolan-5-ones useful in the production of antiviral nucleoside analogues
AU2008202336B2 (en) * 2001-03-01 2011-11-10 Abbvie Inc. Polymorphic and other crystalline forms of cis-FTC
CN102942563A (zh) * 2001-03-01 2013-02-27 基利得科学公司 顺-ftc的多晶型物及其它晶型
PL215267B1 (pl) * 2001-06-15 2013-11-29 Shire Canada Inc Stereoselektywny sposób wytwarzania cis-2-hydroksymetylo-4-(cytozyn-1'-ylo)-1,3-oksatiolanu
US6600044B2 (en) 2001-06-18 2003-07-29 Brantford Chemicals Inc. Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
WO2003051298A2 (en) * 2001-12-14 2003-06-26 Pharmasset Ltd. Preparation of intermediates useful in the synthesis of antiviral nucleosides
AU2003259154B2 (en) * 2002-07-19 2006-12-07 The Regents Of The University Of California Benzimidazole derivatives and their use as prodrugs of proton pump inhibitor
US6855821B2 (en) 2002-08-06 2005-02-15 Pharmasset, Ltd. Processes for preparing 1,3-dioxolane nucleosides
CN105596356A (zh) * 2003-01-14 2016-05-25 吉里德科学公司 用于联合抗病毒治疗的组合物和方法
EP1693482A4 (de) * 2003-12-09 2008-04-30 Asahi Glass Co Ltd Ti-oxid-film mit photokatalytischer aktivität bei bestrahlung mit sichtbarem licht und herstellungsverfahren dafür
EP1720840B1 (de) * 2004-02-03 2016-02-03 Emory University Verfahren zur herstellung von 1,3-dioxolannukleosiden
CA2667891A1 (en) * 2006-10-30 2008-05-08 Lupin Limited An improved process for the manufacture of lamivudine
ES2542154T3 (es) * 2007-09-28 2015-07-31 Avexa Limited Un procedimiento para la resolución quiral de 1,3-oxatiolanos sustituidos en posición 2 y sustituidos en posición 4
EP2048151A1 (de) * 2007-10-10 2009-04-15 Cilag AG Verfahren zur Herstellung von Nukleosiden durch direkte Glykosidation der Nukleosidbase
EP2050757A1 (de) * 2007-10-10 2009-04-22 Cilag AG Verfahren zur Herstellung von 2' -deoxy-5-Azacytidin (Decitabin)
WO2010055526A1 (en) * 2008-11-12 2010-05-20 Lupin Limited A novel polymorph of emtricitabine and a process for preparing of the same
WO2010082128A1 (en) 2009-01-19 2010-07-22 Aurobindo Pharma Limited Process for the preparation of cis-nucleoside derivative
WO2011007367A1 (en) 2009-07-15 2011-01-20 Lupin Limited An improved process for preparation of efavirenz
WO2011141805A2 (en) 2010-05-14 2011-11-17 Lupin Limited An improved process for the manufacture of lamivudine
EP2739620A1 (de) 2011-08-05 2014-06-11 Lupin Limited Stereoselektives verfahren zur herstellung von 1,3-oxathiolan-nukleosiden
CN106478618A (zh) * 2016-10-14 2017-03-08 上海礼泰医药科技有限公司 恩曲他滨氢卤酸盐的制备方法
CN109553610B (zh) * 2018-12-21 2020-10-27 江西富祥药业股份有限公司 一种恩曲他滨异构体的制备方法
CN115043823A (zh) * 2022-06-28 2022-09-13 江苏普信制药有限公司 一种恩曲他滨的合成方法

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6175008B1 (en) 1988-04-11 2001-01-16 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
NZ228645A (en) 1988-04-11 1991-09-25 Iaf Biochem Int 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections
US5466806A (en) 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
US5041449A (en) 1988-04-11 1991-08-20 Iaf Biochem International, Inc. 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections
US5047407A (en) 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
US5914331A (en) 1990-02-01 1999-06-22 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US6069252A (en) 1990-02-01 2000-05-30 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers
US5700937A (en) 1990-02-01 1997-12-23 Emory University Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds
US5204466A (en) * 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5276151A (en) 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
GB9009861D0 (en) * 1990-05-02 1990-06-27 Glaxo Group Ltd Chemical compounds
US5587480A (en) 1990-11-13 1996-12-24 Biochem Pharma, Inc. Substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes with antiviral properties
US5248776A (en) 1990-12-05 1993-09-28 University Of Georgia Research Foundation, Inc. Process for enantiomerically pure β-L-1,3-oxathiolane nucleosides
US5444063A (en) 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
AU9125991A (en) * 1990-12-05 1992-07-08 University Of Georgia Research Foundation, Inc., The Enantiomerically pure beta -l-(-)-1,3-oxathiolane nucleosides
NZ241625A (en) * 1991-02-22 1996-03-26 Univ Emory 1,3-oxathiolane derivatives, anti-viral compositions containing such and method of resolving racemic mixture of enantiomers
GB9104740D0 (en) 1991-03-06 1991-04-17 Wellcome Found Antiviral nucleoside combination
IE920701A1 (en) 1991-03-06 1992-09-09 Wellcome Found Therapeutic nucleosides
IT1244501B (it) 1991-03-22 1994-07-15 Sigma Tau Ind Farmaceuti Derivati amminoacilici e oligopeptidici dell'allopurinolo dotati di attivita' immunostimolante e composizioni farmaceutiche che li contengono
WO1992018517A1 (en) 1991-04-17 1992-10-29 Yale University Method of treating or preventing hepatitis b virus
GB9110874D0 (en) 1991-05-20 1991-07-10 Iaf Biochem Int Medicaments
ZA923641B (en) 1991-05-21 1993-02-24 Iaf Biochem Int Processes for the diastereoselective synthesis of nucleosides
GB9116601D0 (en) 1991-08-01 1991-09-18 Iaf Biochem Int 1,3-oxathiolane nucleoside analogues
GB9311709D0 (en) 1993-06-07 1993-07-21 Iaf Biochem Int Stereoselective synthesis of nucleoside analogues using bicycle intermediate
IL113432A (en) * 1994-04-23 2000-11-21 Glaxo Group Ltd Process for the diastereoselective synthesis of nucleoside analogues
KR100226533B1 (ko) 1994-07-08 1999-10-15 나까니시 히로유끼 열가소성 폴리에스테르수지 조성물
GB9506644D0 (en) 1995-03-31 1995-05-24 Wellcome Found Preparation of nucleoside analogues
GB9525606D0 (en) * 1995-12-14 1996-02-14 Iaf Biochem Int Method and compositions for the synthesis of dioxolane nucleosides with › - configuration
TW318283B (en) 1996-12-09 1997-10-21 United Microelectronics Corp Multi-level read only memory structure and manufacturing method thereof
DE69921829T2 (de) * 1998-08-12 2005-10-27 Gilead Sciences, Inc., Foster City Verfahren zur herstellung von 1,3-oxathiolannukleoside
US9308044B2 (en) 2002-04-08 2016-04-12 Medtronic Ardian Luxembourg S.A.R.L. Methods for therapeutic renal neuromodulation
US9109124B2 (en) 2011-06-01 2015-08-18 Xerox Corporation Solid ink compositions comprising semicrystalline oligomer resins
JP5800924B2 (ja) 2014-01-20 2015-10-28 ファナック株式会社 回転工具の回転振れ及び動バランス調整機構

Also Published As

Publication number Publication date
IL201293A (en) 2011-02-28
KR20070094667A (ko) 2007-09-20
IL141359A0 (en) 2002-03-10
CA2340214C (en) 2007-10-30
RU2004125183A (ru) 2006-01-27
JP2014132026A (ja) 2014-07-17
EP2322518A1 (de) 2011-05-18
US20030144532A1 (en) 2003-07-31
CA2714085C (en) 2013-02-05
CA2563022C (en) 2010-11-23
EP1361223B1 (de) 2005-04-06
KR100856416B1 (ko) 2008-09-04
CA2563022A1 (en) 2000-02-24
JP2009108080A (ja) 2009-05-21
KR101208429B1 (ko) 2012-12-05
MXPA01001552A (es) 2004-08-23
JP2012176974A (ja) 2012-09-13
BR9912951A (pt) 2001-10-02
CA2714085A1 (en) 2000-02-24
EP1361223A1 (de) 2003-11-12
IL201293A0 (en) 2010-05-31
HK1038921A1 (en) 2002-04-04
JP5956492B2 (ja) 2016-07-27
ES2537540T3 (es) 2015-06-09
ES2232169T3 (es) 2005-05-16
CA2340214A1 (en) 2000-02-24
ATE282034T1 (de) 2004-11-15
KR20060063991A (ko) 2006-06-12
US6576776B1 (en) 2003-06-10
IL173745A0 (en) 2006-07-05
WO2000009494A1 (en) 2000-02-24
AU771779B2 (en) 2004-04-01
PT1104415E (pt) 2005-03-31
CN1141305C (zh) 2004-03-10
EP1104415A1 (de) 2001-06-06
AU2004202930A1 (en) 2004-07-29
JP2002522534A (ja) 2002-07-23
DE69921829T2 (de) 2005-10-27
CN1313858A (zh) 2001-09-19
AU2004202930C1 (en) 2008-11-13
JP5203897B2 (ja) 2013-06-05
PT2322518E (pt) 2015-06-08
IL173745A (en) 2010-05-31
JP5547772B2 (ja) 2014-07-16
EP1104415B1 (de) 2004-11-10
RU2439069C2 (ru) 2012-01-10
ATE292631T1 (de) 2005-04-15
AU2004202930B2 (en) 2008-05-08
EP1535921A1 (de) 2005-06-01
EP2322518B1 (de) 2015-02-25
IL141359A (en) 2006-07-05
KR100687194B1 (ko) 2007-02-27
US6215004B1 (en) 2001-04-10
AU5675299A (en) 2000-03-06
RU2244712C2 (ru) 2005-01-20
BR9912951B1 (pt) 2012-01-10
US6939965B2 (en) 2005-09-06
HK1156604A1 (en) 2012-06-15
US6518425B1 (en) 2003-02-11
JP4249393B2 (ja) 2009-04-02
KR20010072428A (ko) 2001-07-31
DE69921829D1 (de) 2004-12-16

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Legal Events

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8332 No legal effect for de