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Title:
A PROCESS FOR PREPARING R-BETA-AMINO PHENYLBUTYRIC ACID DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2010/009630
Kind Code:
A1
Abstract:
Disclosed is a process for preparing chiral pharmaceutical intermediates of R-beta-amino phenylbutyric acid derivatives (I) and the pharmaceutically acceptable salts thereof, which affords the desired object compounds having specific 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 aqueous 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, Piaoyang (No.145 East Renmin Road, Xinpu DistrictLianyungang, Jiangsu 2, 222002, CN)
孙飘扬 (中国江苏省连云港市新浦区人民东路145号, Jiangsu 2, 222002, CN)
CHEN, Yongjiang (No.145 East Renmin Road, Xinpu DistrictLianyungang, Jiangsu 2, 222002, CN)
Application Number:
CN2009/071259
Publication Date:
January 28, 2010
Filing Date:
April 14, 2009
Export Citation:
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Assignee:
JIANGSU HENGRUI MEDICINE CO., LTD. (No.145 East Renmin Road, Xinpu DistrictLianyungang, Jiangsu 2, 222002, CN)
江苏恒瑞医药股份有限公司 (中国江苏省连云港市新浦区人民东路145号, Jiangsu 2, 222002, CN)
SUN, Piaoyang (No.145 East Renmin Road, Xinpu DistrictLianyungang, Jiangsu 2, 222002, CN)
孙飘扬 (中国江苏省连云港市新浦区人民东路145号, Jiangsu 2, 222002, CN)
International Classes:
C07C227/34; C07C227/04; C07B57/00; C07C229/34
Domestic Patent References:
WO2004085661A22004-10-07
WO2004085661A22004-10-07
WO2005020920A22005-03-10
Foreign References:
CN1845674A2006-10-11
CN1371356A2002-09-25
US7385080B22008-06-10
US5296482A1994-03-22
Other References:
J. AM. CHEM. SOC, 1987, pages 5856
J. AM. CHEM. SOC, 1986, pages 7117
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (Level 19, Tower E3 The Towers, Oriental Plaza,No.1, East Chang An Avenue, Dongcheng District, Beijing 8, 100738, CN)
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