Title:
R-β-アミノフェニル酪酸誘導体の調製方法
Document Type and Number:
Japanese Patent JP5395901
Kind Code:
B2
Abstract:
Disclosed is a process for preparing chiral pharmaceutical intermediates of R-beta-amino phenylbutyric acid derivatives (I) and pharmaceutically acceptable salts thereof, which affords the desired object compounds having special optical configuration by chemosynthesis process comprising resolving the optical isomer mixtures of beta-amino phenylbutyric acid derivatives with resolving agent. This process comprises the resolving step of salification in alcoholic solvent or aquesous solution of alcohol with resolving agent of di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%. The R-beta-amino phenylbutyric acid derivatives (I) produced by this process can be better used in synthesizing medicament.
Inventors:
Sun Piao Yang
Chen Yongjien
Yoo Guang Lian
Chen Yongjien
Yoo Guang Lian
Application Number:
JP2011519011A
Publication Date:
January 22, 2014
Filing Date:
April 14, 2009
Export Citation:
Assignee:
JIANGSU HENGRUI MEDICINE CO.,LTD.
International Classes:
C07C227/34; C07C229/36; C07B57/00
Domestic Patent References:
| JP42011933B1 | ||||
| JP2006510608A |
Foreign References:
| WO2007032409A1 | ||||
| WO2004085661A1 |
Other References:
Journal of Medicinal Chemistry,1982年,Vol.25, No.3,p.216-20
Bioorganic & Medicinal Chemistry Letters,2007年,Vol.17, No.7,P.1903-7
Bioorganic & Medicinal Chemistry Letters,2007年,Vol.17, No.7,P.1903-7
Attorney, Agent or Firm:
Xie Takamine
Yasushi Sasaki
Yasushi Sasaki