发明申请
WO2006021885A1 ENANTIOSELECTIVE BIOTRANSFORMATION FOR PREPARATION OF PROTEIN TYROSINE KINASE INHIBITOR INTERMEDIATES
审中-公开
用于制备蛋白酪氨酸激酶抑制剂中间体的生物传感器
- 专利标题: ENANTIOSELECTIVE BIOTRANSFORMATION FOR PREPARATION OF PROTEIN TYROSINE KINASE INHIBITOR INTERMEDIATES
- 专利标题(中): 用于制备蛋白酪氨酸激酶抑制剂中间体的生物传感器
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申请号: PCT/IB2005/002839申请日: 2005-08-15
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公开(公告)号: WO2006021885A1公开(公告)日: 2006-03-02
- 发明人: KUNG, Pei-Pei , MARTINEZ, Carlos, Alberto , TAO, Junhua
- 申请人: PFIZER INC. , KUNG, Pei-Pei , MARTINEZ, Carlos, Alberto , TAO, Junhua
- 申请人地址: 235 East 42nd Street, New York, NY 10017 US
- 专利权人: PFIZER INC.,KUNG, Pei-Pei,MARTINEZ, Carlos, Alberto,TAO, Junhua
- 当前专利权人: PFIZER INC.,KUNG, Pei-Pei,MARTINEZ, Carlos, Alberto,TAO, Junhua
- 当前专利权人地址: 235 East 42nd Street, New York, NY 10017 US
- 代理机构: FULLER, Grover, F., Jr. et al.
- 优先权: US60/605,118 20040826
- 主分类号: C12P7/22
- IPC分类号: C12P7/22 ; C07C33/46 ; C12P41/00
摘要:
The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral ( S )-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.