Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
    10.
    发明授权
    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

    公开(公告)号:US07465842B2

    公开(公告)日:2008-12-16

    申请号:US11213025

    申请日:2005-08-26

    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.

    摘要翻译: 本发明涉及制备1-(2,6-二氯-3-氟苯基)乙醇的对映体纯纯立体异构体的生物催化方法。 公开了制备所需(S) - 对映体的方法,该方法基于酶拆分,化学酯化和化学水解与1-(2,6-二氯-3-氟苯基)乙酯的倒置或立体选择性反应 用生物催化剂如酶或微生物生物还原2,6-二氯-3-氟 - 苯乙酮。 手性(S) - 对映体可用于合成某些对映异构体富集的醚连接的2-氨基吡啶化合物,其有效抑制人类肝细胞生长因子受体的自身磷酸化。