IMPROVEMENT IN THE PRODUCTION OF IMIDAZOLE DERIVATIVES AND NOVEL INTERMEDIATES OF THE DERIVATIVES

Title:

IMPROVEMENT IN THE PRODUCTION OF IMIDAZOLE DERIVATIVES AND NOVEL INTERMEDIATES OF THE DERIVATIVES

Document Type and Number:

WIPO Patent Application WO/2003/070722

Kind Code:

A1

Abstract:

An improvement in the production of imidazole derivatives including histamine H₃ agonist immepip and histamine H₃ antagonist VUF4929. Desired imidazole derivatives can be easily obtained in high yield by using novel intermediates represented by the general formula (I): (I) wherein R¹ is an amino-protecting group; R² and R³ are each independently hydrogen, lower alkyl, or hydroxylated lower alkyl; R⁴ is lower alkyl, halogenated lower alkyl, or substituted or unsubstituted phenyl; and A is C_1-3 alkylene.

Inventors:

SAKAMOTO YASUHIKO (JP)
KURIHARA TAKUSHI (JP)
HARUSAWA SHINYA (JP)

Application Number:

PCT/JP2003/001687

Publication Date:

August 28, 2003

Filing Date:

February 18, 2003

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Assignee:

AZWELL INC (JP)
SAKAMOTO YASUHIKO (JP)
KURIHARA TAKUSHI (JP)
HARUSAWA SHINYA (JP)

International Classes:

C07D401/06; C07F9/6506; (IPC1-7): C07D401/06; C07F9/6506

Foreign References:

US6100264A

2000-08-08

Other References:

ZBIRAL ERICH ET AL.: "A novel approach to (heteroarylmethyl)- and (heteroarylethyl) phosphonates and their free acids", SYNTHESIS, no. 9, 1988, pages 735 - 739, XP002962189
SHIN'YA HARUSAWA ET AL.: "An efficient and convenient synthesis of 4-vinylimidazoles using a novel Horner-Wadsworth-Emmons (HWE), reagent: synthetic studies toward novel histamine H3-ligands", SYNTHESIS, no. 8, 2002, pages 1072 - 1078, XP002962190
See also references of EP 1477487A4

Attorney, Agent or Firm:

Aoyama, Tamotsu (3-7 Shiromi 1-chom, Chuo-ku Osaka-shi Osaka, JP)

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