首页> 外国专利> Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates

Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates

机译:对映选择性生物转化制备蛋白酪氨酸激酶抑制剂中间体

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.
机译:本发明涉及用于制备对映体纯的1-(2,6-二氯-3-氟苯基)乙醇的立体异构体的生物催化方法。公开了所需的(S)-对映异构体的制备方法,该方法基于酶促拆分,化学酯化和化学水解与1-(2,6-二氯-3-氟苯基)乙基酯的转化或立体选择性的组合。用生物催化剂,例如酶或微生物对2,6-二氯-3-氟-苯乙酮进行生物还原。手性(S)-对映异构体可用于合成某些对映异构体富集的,与醚连接的2-氨基吡啶化合物,这些化合物可有效抑制人肝细胞生长因子受体的自磷酸化。

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