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Patent Searching and Data


Title:
IMPROVED METHOD FOR PREPARATION OF REBAMIPIDE
Document Type and Number:
Japanese Patent JP2004131506
Kind Code:
A
Abstract:

To provide a method for preparation of rebamipide which is a therapeutic agent for gastric ulcer, and specified in formula (1).

The method for preparation of rebamipide specified in formula (1) comprises a step reacting a halomethylcarbostyryl compound and diethylmalonate and then adding a base to the reaction product to produce an acetylcarbostyryl compound by decarboxylation, a step producing a carbostyrylamino acid compound by deprotecting the acetylcarbostyryl compound in a mixture of hydrochloric acid-acetic acid, and an acylation step. The method allows an easy preparation of the rebamipide specified in formula (1) in a mild condition with high yield and purity as compared to conventional methods.


Inventors:
BUN EIGO
KA TAIGI
KIM KOSEN
LEE JAE CHUL
LEE SOTETSU
CHO EIKITSU
LEE KANJUN
Application Number:
JP2003353221A
Publication Date:
April 30, 2004
Filing Date:
October 14, 2003
Export Citation:
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Assignee:
HANMI PHARM IND CO LTD
International Classes:
C07D215/22; C07B61/00; C07D215/14; (IPC1-7): C07D215/22
Attorney, Agent or Firm:
Takehiko Suzue
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto