Title:
A METHOD FOR PREPARING FLUTICASONE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2003/013427
Kind Code:
A2
Abstract:
A method for preparing 6&agr ,9&agr -difluoro-17&agr -[(2-furanylcarbonyl)oxy]-11ß-hydroxy-16&agr -methyl-3-oxoandrosta-1,4-diene-17ß-carbothioicacid S-fluoromethyl ester from a thiocarboxylic acid by reacting the thiocarboxylic acid with a solution containing chlorofluoromethane and a mild base medium at a temperature in the range of -60° C to 90° C.
Inventors:
PARTRIDGE JOHN JOSEPH (US)
WALKER DWIGHT SHEROD (US)
WALKER DWIGHT SHEROD (US)
Application Number:
PCT/US2002/024586
Publication Date:
February 20, 2003
Filing Date:
August 01, 2002
Export Citation:
Assignee:
SMITHKLINE BEECHAM CORP (US)
PARTRIDGE JOHN JOSEPH (US)
WALKER DWIGHT SHEROD (US)
PARTRIDGE JOHN JOSEPH (US)
WALKER DWIGHT SHEROD (US)
International Classes:
A61P11/00; A61P11/02; A61P11/06; A61P17/06; A61P19/02; A61P27/14; A61P37/08; C07J31/00; (IPC1-7): A61K/
Domestic Patent References:
| WO2001062722A2 | 2001-08-30 |
Foreign References:
| US4093721A | 1978-06-06 | |||
| US3989686A | 1976-11-02 | |||
| US4335121A | 1982-06-15 |
Other References:
DATABASE CAPLUS [Online] CHERKEZ S.: 'Process for the manufacture of androstane-17-carbothiolates via esterification with halofluoromethanes', XP002963386 Retrieved from STN Database accession no. 1998:706263 & IL 109 656 A1 22 February 1998
PHILLIPPS ET AL.: 'Synthesis and structure-activity relationships in a series of antiinflammatory corticosteroid analogues, halomethyl androstane-17-beta carbothioates and 17-beta-carboselenoates' J. OF MEDICINAL CHEMISTRY vol. 37, no. 22, 01 October 1994, pages 3717 - 3729, XP002025925
PHILLIPPS ET AL.: 'Synthesis and structure-activity relationships in a series of antiinflammatory corticosteroid analogues, halomethyl androstane-17-beta carbothioates and 17-beta-carboselenoates' J. OF MEDICINAL CHEMISTRY vol. 37, no. 22, 01 October 1994, pages 3717 - 3729, XP002025925
Attorney, Agent or Firm:
Levy, David J. (Corporate Intellectual Property Department
Five Moore Drive, PO Box 1339, Research Triangle Park NC, US)
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