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

Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
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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