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Title:
PROCESSES FOR PREPARATION OF TETRAHYDRONAPHTHALENE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2002/042243
Kind Code:
A1
Abstract:
Processes for preparing optically active intermediates for the synthesis of tetrahydronaphthalene derivatives useful as PGI¿2? agonist can be provided by providing a method for optical resolution of a tetrahydronaphthalene derivative of the following general formula with a reagent for optical resolution and a method for inversion of such a derivative at its asymmetric center. In the formula, R?1¿ is a hydroxyl-protecting group; R?2¿ is hydrogen or halogeno; R?3¿ is hydrogen, hydroxyl, or protected hydroxyl; and R?4¿ is hydrogen, hydroxyl, protected hydroxyl, lower alkyl, or halogeno.

Inventors:
ICHIHARA MASAHARU (JP)
HASHIMOTO NORIO (JP)
OHIGASHI ATSUSHI (JP)
KANDA ATSUSHI (JP)
KAGARA KOOJI (JP)
MORIKI SHIGERU (JP)
BABA YUKIHISA (JP)
Application Number:
PCT/JP2001/009861
Publication Date:
May 30, 2002
Filing Date:
November 12, 2001
Export Citation:
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Assignee:
FUJISAWA PHARMACEUTICAL CO (JP)
ICHIHARA MASAHARU (JP)
HASHIMOTO NORIO (JP)
OHIGASHI ATSUSHI (JP)
KANDA ATSUSHI (JP)
KAGARA KOOJI (JP)
MORIKI SHIGERU (JP)
BABA YUKIHISA (JP)
International Classes:
C07B57/00; (IPC1-7): C07B57/00; C07B53/00; C07B55/00; C07C37/01; C07C39/38; C07C41/26; C07C41/32; C07C43/23
Domestic Patent References:
WO2000078350A12000-12-28
WO1995024393A11995-09-14
Foreign References:
JPH09187292A1997-07-22
JPH07196565A1995-08-01
JPH04211074A1992-08-03
Other References:
RUANO JOSE L. GARCIA ET AL.: "A new stereo-controlled entry into the anthracyclinone families. Part 1. Synthesis of bicyclic precursors of 4-demethoxy-7-deoxy-derivatives", TETRAHEDRON ASYMMETRY, vol. 10, no. 15, 1999, pages 2935 - 2944, XP004179149
KIM HEE-DOO ET AL.: "A novel synthetic route to 11-deoxyanthracycline AB synthons", ARCH. PHARMACOL. RES., vol. 17, no. 4, 1994, pages 249 - 255, XP002908284
IZAWA TOSHIO ET AL.: "A novel enantiocontrolled synthesis of (+)-9-deacetyl-9-(hydroxymethyl)-4-demethoxydaunomycinone", CHEM. LETT., no. 8, 1987, pages 1655 - 1656, XP002908285
COREY E.J. ET AL.: "Short enantioselective synthesis of (-)-ovalicin, a potent inhibitor of angiogenesis, using substrate-enhanced catalytic asymmetric dihydroxylation", J. AM. CHEM. SOC., vol. 116, no. 26, 1994, pages 12109 - 12110, XP002908286
Attorney, Agent or Firm:
Tabushi, Eiji c/o Fujisawa Pharmaceutical Co. (Ltd. Osaka Factory 1-6 Kashima 2-chom, Yodogawa-ku Osaka-shi Osaka, JP)
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