发明授权
US07465842B2 Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
失效
用于制备蛋白酪氨酸激酶抑制剂中间体的对映选择性生物转化
- 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对映选择性生物转化
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申请号: US11213025申请日: 2005-08-26
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公开(公告)号: US07465842B2公开(公告)日: 2008-12-16
- 发明人: Pei-Pei Kung , Carlos Martinez , Junhua Tao
- 申请人: Pei-Pei Kung , Carlos Martinez , Junhua Tao
- 申请人地址: US CA San Diego
- 专利权人: Agouron Pharmaceuticals, Inc.
- 当前专利权人: Agouron Pharmaceuticals, Inc.
- 当前专利权人地址: US CA San Diego
- 代理商 Bryan C. Zielinski; Galina M. Yakovleva
- 主分类号: C07C21/18
- IPC分类号: C07C21/18 ; C07C25/08 ; C07C25/00 ; 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.
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