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Title:
PROCESS FOR PREPARING [(S)-(-)ALPHA-METHYLAMINO PHENYLACETONE]2 (2R, 3R)-TARTARIC ACID DERIVATES
Document Type and Number:
WIPO Patent Application WO/2005/118524
Kind Code:
A1
Abstract:
A preparation method of [(S)-(-)-alpha-methylamino phenylacetone ]2 (2R,3R)­-tartaric acid derivates is disclosed, which comprises forming salt from (±) -alpha­methylamino phenylacetone, (R)-(+)-alpha-methylamino phenylacetone or (±) - alpha-methylamino phenylacetone doped with partial (S)-(-)-alpha-methylamino phenylacetone and (2R,3R)-tartaric acid derivates in solvent, separating [(S)-(-)­alpha-methylamino phenylacetone]2 (2R,3R)-tartaric acid derivates in mixed solvents by controlling the ratio and total amount of the mixed solvents, collecting object product from reaction product by using general method. The resoluted product has high optical yield and optical purity, and can be directly used for synthesizing (1R,2S)-(-)-ephedrine. A method for racemating (R)-(-)-alpha-methylamino phenylacetone by directly heating without additionally adding acid or base is also disclosed.

Inventors:
Huang, Chengjun (1320, Beijing Road, Shanghai 0, 20004, W)
Zhou, Houyuan (1320, Beijing Road, Shanghai 0, 20004, W)
Application Number:
PCT/CN2005/000744
Publication Date:
December 15, 2005
Filing Date:
May 27, 2005
Export Citation:
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Assignee:
Shanghai, Institute Pharmaceutical Industry OF. (1320, Beijing Road, Shanghai 0, 20004, W)
ZHEJIANG KANGYU PHARMACEUTICAL CO., LTD. (8 Jiangnan West Road, Hengdian Village Dongyang, Zhejiang 8, 32211, CN)
Huang, Chengjun (1320, Beijing Road, Shanghai 0, 20004, W)
Zhou, Houyuan (1320, Beijing Road, Shanghai 0, 20004, W)
International Classes:
C07C221/00; C07C225/16; (IPC1-7): C07C225/16; C07C221/00; C07M7/00
Foreign References:
US2802865A
CN1298867A
CN1267664A
CN1265391A
US5227526A
Attorney, Agent or Firm:
CHINA SINDA INTELLECTUAL PROPERTY LTD. (B11th Floor, Focus Place 19 Financial Street, Beijing 2, 10003, CN)
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