Title:
PROCESS FOR THE PREPARATION OF FLUORINATED DERIVATIVES OF NUCLEOSIDES OR SUGARS
Document Type and Number:
WIPO Patent Application WO/2000/039144
Kind Code:
A1
Abstract:
A process for efficiently preparing nucleoside or sugar derivatives whose secondary hydroxyl groups are selectively replaced by fluorine atoms, which comprises reacting a nucleoside or sugar derivative bearing secondary hydroxyl groups with a sulfonyl fluoride such as a perfluoroalkanesulfonyl fluoride or alkanesulfonyl fluoride in the presence of a base. This process is an uncostly, safe and industrially advantageous one permitting one-step fluorination of the above hydroxyl groups, thus being extremely useful for the preparation of intermediates for various drugs including antivirals.
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Inventors:
TAKAMATSU SATOSHI (JP)
KATAYAMA SATOSHI (JP)
HIROSE NAOKO (JP)
IZAWA KUNISUKE (JP)
DECOCK ETIENNE (BE)
DEMILLEQUAND MARC (BE)
SCHELKENS GEERT (BE)
BREPOELS JOZEF (BE)
KATAYAMA SATOSHI (JP)
HIROSE NAOKO (JP)
IZAWA KUNISUKE (JP)
DECOCK ETIENNE (BE)
DEMILLEQUAND MARC (BE)
SCHELKENS GEERT (BE)
BREPOELS JOZEF (BE)
Application Number:
PCT/JP1999/006500
Publication Date:
July 06, 2000
Filing Date:
November 24, 1999
Export Citation:
Assignee:
AJINOMOTO KK (JP)
TAKAMATSU SATOSHI (JP)
KATAYAMA SATOSHI (JP)
HIROSE NAOKO (JP)
IZAWA KUNISUKE (JP)
DECOCK ETIENNE (BE)
DEMILLEQUAND MARC (BE)
SCHELKENS GEERT (BE)
BREPOELS JOZEF (BE)
TAKAMATSU SATOSHI (JP)
KATAYAMA SATOSHI (JP)
HIROSE NAOKO (JP)
IZAWA KUNISUKE (JP)
DECOCK ETIENNE (BE)
DEMILLEQUAND MARC (BE)
SCHELKENS GEERT (BE)
BREPOELS JOZEF (BE)
International Classes:
C07H1/00; C07H9/04; C07H19/04; C07H19/16; (IPC1-7): C07H19/06; C07H19/16
Foreign References:
| JPH11217396A | 1999-08-10 | |||
| EP0495225A1 | 1992-07-22 |
Other References:
MAQBOOL A. SIDDIQUI ET. AL.: 'A New Synthetic Approach to the Clinically Useful, Anti-HIV-Active Nucleoside, 9-(2,3-Dideoxy-2-fluoro-beta-D-threo-pentof uranosyl) adenine (beta-FddA). Introduction of a 2'-beta-Fluoro Substituent via Inversion of a Really Obtainable 2'-alpha-Fluoro Isomer' TETRAHEDRON LETTERS vol. 39, no. 13, 26 March 1998, pages 1657 - 1660, XP002926079
VICTOR E. MARQUEZ, ET. AL.: 'Acid-Stable 2'-Fluoro Purine Dideoxynucleosides as Active Agents against HIV.' J. MED. CHEM. vol. 33, no. 3, March 1990, pages 978 - 985, XP002926080
VICTOR E. MARQUEZ, ET. AL.: 'Acid-Stable 2'-Fluoro Purine Dideoxynucleosides as Active Agents against HIV.' J. MED. CHEM. vol. 33, no. 3, March 1990, pages 978 - 985, XP002926080
Attorney, Agent or Firm:
Ishida, Yasumasa (7th floor 20-12 Shin-Yokohama 3-chome Kohoku-ku, Yokohama-shi Kanagawa, JP)
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