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Title:
PROCESS FOR PRODUCING 4-METHYL-1,3-THIAZOL-2-YLSULFONYL HALIDE
Document Type and Number:
WIPO Patent Application WO/2004/022549
Kind Code:
A1
Abstract:
A process for producing a compound represented by the formula (I) (wherein X represents halogeno), characterized by using 4-methyl-1,3-thiazole as a starting material and using a Grignard reagent (an alkylmagnesium halide or arylmagnesium halide) in the presence of sulfur dioxide and a halogenating agent. (I) By this process, the compound represented by the formula (I), which has an antagonistic effect against a PGE2 subtype EP1 receptor and is an intermediate for medicines, can be mass-synthesized through a safe anionic reaction at a temperature of -20 to 10°C.

Inventors:
KASAMATSU EIJI (JP)
NISHITA YOSHITAKA (JP)
NAGANAWA ATSUSHI (JP)
Application Number:
PCT/JP2003/011418
Publication Date:
March 18, 2004
Filing Date:
September 08, 2003
Export Citation:
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Assignee:
ONO PHARMACEUTICAL CO (JP)
KASAMATSU EIJI (JP)
NISHITA YOSHITAKA (JP)
NAGANAWA ATSUSHI (JP)
International Classes:
C07D277/36; (IPC1-7): C07D277/36
Domestic Patent References:
WO1995023809A11995-09-08
WO1995029904A11995-11-09
WO2002072564A12002-09-19
Foreign References:
EP0511826A21992-11-04
Other References:
ROBLIN RICHARD O.: "THE PREPARATION OF HETEROCYCLIC SULFONAMIDES", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 72, 1950, pages 4890 - 4892, XP002974646
FEIT B-A: "A HYDRIDE TRANSFER REACTION FROM SALTS OF CARBANIONS TO ACTIVATED OLEFINS", TETRAHEDRON, vol. 51, no. 1, 1995, pages 317 - 328, XP004104968
Attorney, Agent or Firm:
Ohie, Kunihisa (Horiguchi No.2 Bldg. 7F 2-6, Nihonbashi-Ningyocho, 2-chom, Chuo-ku Tokyo, JP)
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