PROCESS FOR PRODUCING COMPOUND HAVING NK1 RECEPTOR ANTAGONISM AND PRODUCTION INTERMEDIATE THEREOF

Title:

PROCESS FOR PRODUCING COMPOUND HAVING NK1 RECEPTOR ANTAGONISM AND PRODUCTION INTERMEDIATE THEREOF

Document Type and Number:

WIPO Patent Application WO/2005/019225

Kind Code:

A1

Abstract:

A process for producing 2-(4-acetylpiperazin-1-yl)-6-[3,5-bis(trifluoromethyl)phenylmethyl]-4-(2-methylphenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one (compound 1) for industrial production of a compound having excellent antagonism against tachykinin receptor, especially NK1 receptor antagonism. The process is characterized by comprising causing a chlorinating agent to act on 4-(2-methylphenyl)-2-methylthio-6-oxo-1,6-dihydro-5-pyrimidinecarboxylic acid (7) as an intermediate; reacting the product with 3-[3,5-bis(trifluoromethyl)benzylamino]-1-propanol; causing a base to act on the product to thereby effect cyclization; effecting oxidation thereof; and reacting the oxide with N-acetylpiperazine.

Inventors:

ARAYA ICHIRO (JP)
KANAZAWA SHINTARO (JP)

Application Number:

PCT/JP2004/011965

Publication Date:

March 03, 2005

Filing Date:

August 20, 2004

Export Citation:

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Assignee:

KYORIN SEIYAKU KK (JP)
ARAYA ICHIRO (JP)
KANAZAWA SHINTARO (JP)

International Classes:

A61K31/519; A61P43/00; C07D493/04; (IPC1-7): C07D498/04; A61K31/519; A61P43/00; C07D239/56

Domestic Patent References:

WO2003062245A1	2003-07-31
WO2001007027A2	2001-02-01

Foreign References:

JPH09263585A	1997-10-07
JP2002541259A	2002-12-03

Other References:

HAMPER B C ET AL: "Solid phase synthesis of dihydropyrimidinones and pyrimidinone carboxylic acids from malonic acid resin", TETRAHEDRON LETTERS, vol. 40, no. 27, 2 July 1999 (1999-07-02), pages 4973 - 7976, XP004169373

Attorney, Agent or Firm:

Kishida, Masayuki (Marunouchi-Yaesu Building 6-2, Marunouchi 2-chom, Chiyoda-ku Tokyo 05, JP)

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