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WO2008107771A3 - 2',3'-di-o-acyl-5-fluoronucleosides - Google Patents

2',3'-di-o-acyl-5-fluoronucleosides Download PDF

Info

Publication number
WO2008107771A3
WO2008107771A3 PCT/IB2008/000482 IB2008000482W WO2008107771A3 WO 2008107771 A3 WO2008107771 A3 WO 2008107771A3 IB 2008000482 W IB2008000482 W IB 2008000482W WO 2008107771 A3 WO2008107771 A3 WO 2008107771A3
Authority
WO
WIPO (PCT)
Prior art keywords
fluoronucleosides
acyl
deoxy
intermediates
useful
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.)
Ceased
Application number
PCT/IB2008/000482
Other languages
French (fr)
Other versions
WO2008107771A2 (en
Inventor
Massimo Pregnolato
Marco Terreni
Daniela Ubiali
Teodora Bavaro
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.)
INNOVATE BIOTECHNOLOGY Srl
Original Assignee
INNOVATE BIOTECHNOLOGY Srl
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 INNOVATE BIOTECHNOLOGY Srl filed Critical INNOVATE BIOTECHNOLOGY Srl
Priority to EP08719215A priority Critical patent/EP2176278A2/en
Publication of WO2008107771A2 publication Critical patent/WO2008107771A2/en
Publication of WO2008107771A3 publication Critical patent/WO2008107771A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Saccharide Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)

Abstract

The invention concerns new 2',3'-di-O-acyl-5-fluoronucleosides of formula (I) useful as intermediates in the preparation of 5'-deoxy-2',3'-di-O-acyl-5-fluoronucleosides.
PCT/IB2008/000482 2007-03-05 2008-03-04 2',3'-di-o-acyl-5-fluoronucleosides Ceased WO2008107771A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP08719215A EP2176278A2 (en) 2007-03-05 2008-03-04 2',3'-di-o-acyl-5-fluoronucleosides

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2007A000435 2007-03-05
ITMI20070435 ITMI20070435A1 (en) 2007-03-05 2007-03-05 2 ', 3'-DI-O-acyl-5-FLUORONUCLEOSIDI

Publications (2)

Publication Number Publication Date
WO2008107771A2 WO2008107771A2 (en) 2008-09-12
WO2008107771A3 true WO2008107771A3 (en) 2008-10-30

Family

ID=39642969

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2008/000482 Ceased WO2008107771A2 (en) 2007-03-05 2008-03-04 2',3'-di-o-acyl-5-fluoronucleosides

Country Status (3)

Country Link
EP (1) EP2176278A2 (en)
IT (1) ITMI20070435A1 (en)
WO (1) WO2008107771A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101993464B (en) * 2009-08-19 2014-07-23 成都弘达药业有限公司 Preparation method of capecitabine
CN102212095B (en) * 2010-04-08 2016-03-30 上海医药工业研究院 The preparation method of capecitabine and intermediate thereof
CN102424697B (en) * 2011-10-27 2014-02-12 齐鲁天和惠世制药有限公司 2',3'- di-O-acetyl-5'-deoxy-5-fulurocytidineonium compound and preparation method thereof
CN103897004B (en) * 2012-12-27 2017-05-31 鲁南制药集团股份有限公司 Synthesis method of capecitabine
CN112876526A (en) * 2021-01-15 2021-06-01 山东铂源药业有限公司 Preparation method of capecitabine key intermediate

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003057894A1 (en) * 2002-01-14 2003-07-17 Innovate Biotechnology S.R.L. Process for the selective enzymatic hydrolysis of nucleoside polyesters
US20050137392A1 (en) * 2003-12-22 2005-06-23 Roche Colorado Corporation Process for producing N4-Acyl-5'-deoxy-5-fluorocytidine

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1327358C (en) 1987-11-17 1994-03-01 Morio Fujiu Fluoro cytidine derivatives
DK638688D0 (en) 1988-11-16 1988-11-16 Novo Industri As PARTICULAR IMMOBILIZED LIPASE PREPARATION, PROCEDURE FOR PREPARING IT AND USING THEREOF
US5182201A (en) 1990-10-26 1993-01-26 Uop Lipase immobilization without covalent bonding on an amphiphilic support containing lipophilic alkyl chains
AT398310B (en) 1991-08-30 1994-11-25 Chemie Linz Gmbh IMMOBILIZED LIPASE, METHOD FOR THE PRODUCTION THEREOF AND METHOD FOR INCREASING THE ENANTIOSELECTIVITY OF A CANDIDA LIPASE IN THE Esterification of CHIRAL ALCOHOLS
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
DE4408152A1 (en) 1994-03-11 1995-09-14 Studiengesellschaft Kohle Mbh Immobilized lipases in hydrophobic sol-gel materials
US5476932A (en) 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003057894A1 (en) * 2002-01-14 2003-07-17 Innovate Biotechnology S.R.L. Process for the selective enzymatic hydrolysis of nucleoside polyesters
US20050137392A1 (en) * 2003-12-22 2005-06-23 Roche Colorado Corporation Process for producing N4-Acyl-5'-deoxy-5-fluorocytidine

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KWAN-HEE KIM ET AL: "Synthesis and Biological Activity of the New 5-Fluorocytosine Derivatives, 5'-Deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-carboxylic Acid", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 12, 2002, pages 483 - 486, XP001154721 *
NOBUO SHIMMA ET AL: "The Design and Synthesis of a New Tumor-Selective Fluoropyrimidine Carbamate, Capecitadine", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 8, 2000, pages 1697 - 1706, XP002329188 *

Also Published As

Publication number Publication date
EP2176278A2 (en) 2010-04-21
ITMI20070435A1 (en) 2008-09-06
WO2008107771A2 (en) 2008-09-12

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