INTERMEDIATE OF 6-SUBSTITUTED-1-METHYL-1-H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR PRODUCING SAME

WIPO Patent Application WO/2006/035685

A1

Disclosed are novel production intermediates (IIa) and (III) of a 6-substituted-1-methyl-1-H-benzimidazole derivative (I) as a publicly-known pharmaceutically active ingredient. Also disclosed is a production method suitable for mass synthesis of N-(5-substituted-2-nitrophenyl)-N-methylamines (II) as production intermediates. Further disclosed is a method for efficiently producing a 6-substituted-1-methyl-1-H-benzimidazole derivative (I) from a production intermediate (II) through a short process. The present invention relates to a method for producing a compound (I) represented by the formula below and a production intermediate of the compound (I). (III) (I) (In the formula, R² represents a phenyl group which may have a substituent such as a C₁-C₆ alkyl group or the like, and X represents an oxygen atom, a sulfur atom or a nitrogen atom.)

OKAZAKI REI
IKEUCHI YUTAKA
KAJINO HISAKI
MIYAMOTO HIROSHI

PCT/JP2005/017573

April 06, 2006

September 26, 2005

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SANKYO CO (JP)
OKAZAKI REI
IKEUCHI YUTAKA
KAJINO HISAKI
MIYAMOTO HIROSHI

C07C217/84; C07C209/10; C07C211/52; C07C213/00; C07C271/28; C07D277/20; C07D277/34; C07D417/12

JP2004517080A	2004-06-10
JP2003238406A	2003-08-27
JPS6440449A	1989-02-10
JPH09295970A	1997-11-18
JPH11193276A	1999-07-21
EP1022272A1	2000-07-26
EP0385850A2	1990-09-05

JOURNAL OF MEDICINAL CHEMISTRY, vol. 39, 1996, pages 3971 - 3979
See also references of EP 1798216A4

Yaguchi, Toshiaki c/o SANKYO COMPANY (LIMITED 2-58, Hiromachi 1-chom, Shinagawa-ku Tokyo, JP)

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