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    Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
    1.
    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

    申请人： Pei-Pei Kung ,  Carlos Martinez ,  Junhua Tao

    发明人： Pei-Pei Kung ,  Carlos Martinez ,  Junhua Tao

    IPC分类号： C07C21/18 ,  C07C25/08 ,  C07C25/00 ,  C12P41/00

    CPC分类号： C12P41/004 ,  C07B2200/07 ,  C07C33/46 ,  C12P7/22

    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。

    Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates
    2.
    发明申请
    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：US20060046287A1

    公开(公告)日：2006-03-02

    申请号：US11213025

    申请日：2005-08-26

    申请人： Pei-Pei Kung ,  Carlos Martinez ,  Junhua Tao

    发明人： Pei-Pei Kung ,  Carlos Martinez ,  Junhua Tao

    IPC分类号： C12P7/62 ,  C12P7/22

    CPC分类号： C12P41/004 ,  C07B2200/07 ,  C07C33/46 ,  C12P7/22

    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。