DE69401045D1 - Stereoselektives Verfahren zur Herstellung von Beta-Anomer angereicherten 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy-geschützten 1-alkyl und aryl-sulfonat-Zwischenprodukten - Google Patents

Stereoselektives Verfahren zur Herstellung von Beta-Anomer angereicherten 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy-geschützten 1-alkyl und aryl-sulfonat-Zwischenprodukten

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Publication number
DE69401045D1
DE69401045D1 DE69401045T DE69401045T DE69401045D1 DE 69401045 D1 DE69401045 D1 DE 69401045D1 DE 69401045 T DE69401045 T DE 69401045T DE 69401045 T DE69401045 T DE 69401045T DE 69401045 D1 DE69401045 D1 DE 69401045D1
Authority
DE
Germany
Prior art keywords
ribofuranosyl
deoxy
difluoro
alkyl
beta
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 - Fee Related
Application number
DE69401045T
Other languages
English (en)
Other versions
DE69401045T2 (de
Inventor
Charles David Jones
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of DE69401045D1 publication Critical patent/DE69401045D1/de
Application granted granted Critical
Publication of DE69401045T2 publication Critical patent/DE69401045T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H11/00Compounds containing saccharide radicals esterified by inorganic acids; Metal salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DE69401045T 1993-08-25 1994-08-24 Stereoselektives Verfahren zur Herstellung von Beta-Anomer angereicherten 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy-geschützten 1-alkyl und aryl-sulfonat-Zwischenprodukten Expired - Fee Related DE69401045T2 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/111,578 US5424416A (en) 1993-08-25 1993-08-25 Process for preparation of 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonates and their use in preparation of 2',2'-difluoro-2'-deoxy nucleosides

Publications (2)

Publication Number Publication Date
DE69401045D1 true DE69401045D1 (de) 1997-01-16
DE69401045T2 DE69401045T2 (de) 1997-04-10

Family

ID=22339311

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69401045T Expired - Fee Related DE69401045T2 (de) 1993-08-25 1994-08-24 Stereoselektives Verfahren zur Herstellung von Beta-Anomer angereicherten 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy-geschützten 1-alkyl und aryl-sulfonat-Zwischenprodukten

Country Status (9)

Country Link
US (1) US5424416A (de)
EP (1) EP0640614B1 (de)
JP (1) JP3659989B2 (de)
AT (1) ATE145916T1 (de)
CA (1) CA2130618C (de)
DE (1) DE69401045T2 (de)
DK (1) DK0640614T3 (de)
ES (1) ES2094623T3 (de)
GR (1) GR3022477T3 (de)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521294A (en) * 1995-01-18 1996-05-28 Eli Lilly And Company 2,2-difluoro-3-carbamoyl ribose sulfonate compounds and process for the preparation of beta nucleosides
KR100954390B1 (ko) * 1998-02-25 2010-04-26 에모리 유니버시티 2'-플루오로뉴클레오사이드
US6949522B2 (en) 2001-06-22 2005-09-27 Pharmasset, Inc. β-2′- or 3′-halonucleosides
US6884880B2 (en) * 2002-08-21 2005-04-26 Ash Stevens, Inc. Process for the preparation of 9-β-anomeric nucleoside analogs
US7214791B2 (en) * 2004-07-01 2007-05-08 Shenzhen Hande Technology Co., Ltd. Method for preparation of 2′-deoxy-2′, 2′-difluoro-β-cytidine or pharmaceutically acceptable salts thereof by using 1,6-anhydro-β-d-glucose as raw material
EP1812457A1 (de) * 2004-07-30 2007-08-01 Pharmaessentia Corp. Stereoselektive synthese von b-nukleosiden
WO2006119347A1 (en) * 2005-05-02 2006-11-09 Pharmaessentia Corp. STEREOSELECTIVE SYNTHESIS OF β-NUCLEOSIDES
US8895531B2 (en) * 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
AU2008323923A1 (en) * 2007-11-06 2009-05-14 Pharmaessentia Corporation Novel synthesis of beta-nucleosides
US20090274686A1 (en) * 2008-05-02 2009-11-05 Yat Sun Or Nucleoside phosphonate derivatives

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3282921A (en) * 1964-06-04 1966-11-01 Syntex Corp Halo-deoxynucleosides and processes for the preparation thereof
DE2628202A1 (de) * 1976-06-23 1977-12-29 Max Planck Gesellschaft Verfahren zur herstellung von 2'-substituierten-d-ribofuranosylpurinderivaten
US4211773A (en) * 1978-10-02 1980-07-08 Sloan Kettering Institute For Cancer Research 5-Substituted 1-(2'-Deoxy-2'-substituted-β-D-arabinofuranosyl)pyrimidine nucleosides
FR2531962B1 (fr) * 1982-08-17 1986-11-14 Sandoz Sa Nouveaux derives de la desoxyuridine, leur preparation et leur utilisation comme medicaments
US4526988A (en) * 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
US4625020A (en) * 1983-11-18 1986-11-25 Bristol-Myers Company Nucleoside process
IL77133A (en) * 1984-12-04 1991-01-31 Lilly Co Eli Antineoplastic pharmaceutical compositions containing pentofuranoside derivatives,some new such compounds and their preparation
CA1295998C (en) * 1985-07-29 1992-02-18 Sai P. Sunkara Nucleosides and their use as antineoplastic agents
US4751221A (en) * 1985-10-18 1988-06-14 Sloan-Kettering Institute For Cancer Research 2-fluoro-arabinofuranosyl purine nucleosides
US4965374A (en) * 1987-08-28 1990-10-23 Eli Lilly And Company Process for and intermediates of 2',2'-difluoronucleosides
EP0339161A1 (de) * 1988-04-01 1989-11-02 Merrell Dow Pharmaceuticals Inc. Derivate von Fluorphosphonat-Nukleotiden
JPH0232093A (ja) * 1988-06-08 1990-02-01 Merrell Dow Pharmaceut Inc 抗レトロウィルスジフルオロ化ヌクレオシド類
HU906976D0 (en) * 1989-11-13 1991-05-28 Bristol Myers Squibb Co Process for producing 2', 3'-didesoxy-2'-fluoarabinonucleoside analogues
UA41261C2 (uk) * 1992-06-22 2001-09-17 Елі Ліллі Енд Компані Спосіб одержання збагачених бета-аномером нуклеозидів
US5256798A (en) * 1992-06-22 1993-10-26 Eli Lilly And Company Process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates
US5401861A (en) * 1992-06-22 1995-03-28 Eli Lilly And Company Low temperature process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates

Also Published As

Publication number Publication date
EP0640614A2 (de) 1995-03-01
CA2130618A1 (en) 1995-02-26
JP3659989B2 (ja) 2005-06-15
EP0640614B1 (de) 1996-12-04
JPH07165782A (ja) 1995-06-27
CA2130618C (en) 2006-02-14
DK0640614T3 (da) 1997-04-14
GR3022477T3 (en) 1997-05-31
ES2094623T3 (es) 1997-01-16
ATE145916T1 (de) 1996-12-15
EP0640614A3 (de) 1995-05-03
DE69401045T2 (de) 1997-04-10
US5424416A (en) 1995-06-13

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Legal Events

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8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee