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    Process of making an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonate and use thereof for making a beta nucleoside
    21.
    发明授权
    Process of making an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonate and use thereof for making a beta nucleoside 有权
    制备富含α-脱水异构体的2-脱氧-2,2-二氟-D-呋喃核糖基磺酸盐的方法及其制备β核苷的用途

    公开(公告)号：US07572898B2

    公开(公告)日：2009-08-11

    申请号：US11439664

    申请日：2006-05-24

    申请人： Lung-Hu Wang ,  George Schloemer ,  Allen Liu

    发明人： Lung-Hu Wang ,  George Schloemer ,  Allen Liu

    IPC分类号： C07H15/00

    CPC分类号： C07H19/00 ,  C07H19/048 ,  C07H19/073 ,  C07H19/12 ,  C07H19/22 ,  Y02P20/55

    摘要： A process of preparing an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate, which is useful as an intermediate in the preparation of a beta nucleoside, such as gemcitabine, an anti-tumor agent. A beta-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate is heated and converted to an alpha-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate in the absence of an effective amount of a sulfonate salt to facilitate the conversion. In addition, an anomeric mixture of an alpha-anomer and a beta-anomer of 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate can be dissolved in a mixture of water and a solvent and heated to produce a lactol, which may be further converted to an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate.

    摘要翻译： 制备富含α-脱水异构体的2-脱氧-2,2-二氟-D-核糖核酸磺酸的方法，其可用作制备β核苷的中间体，例如吉西他滨，抗肿瘤剂。 在不存在有效量的磺酸盐的情况下，将β-2-脱氧-2,2-二氟-D-核糖核酸磺酸酯加热并转化成α-2-脱氧-2,2-二氟-D-核糖核酸磺酰基磺酸盐 以方便转换。 此外，可以将2-脱氧-2,2-二氟-D-核糖核酸磺酸的α-端基异构体和β-端基异头体的端基异构体混合物溶解在水和溶剂的混合物中，并加热产生内酯， 可进一步转化为富含α-脱水异构体的2-脱氧-2,2-二氟-D-核糖核酸磺酰基磺酸酯。

    Process of making an alpha-anomer enriched 2-deoxy-2,2-diflouro-d-ribofuranosyl sulfonate and use thereof for making a beta nucleoside
    23.
    发明申请
    Process of making an alpha-anomer enriched 2-deoxy-2,2-diflouro-d-ribofuranosyl sulfonate and use thereof for making a beta nucleoside 有权
    制备富含2-脱氧-2,2-二氟-D-呋喃核糖基磺酸的α-异头物的方法及其制备β核苷的用途

    公开(公告)号：US20060276638A1

    公开(公告)日：2006-12-07

    申请号：US11439664

    申请日：2006-05-24

    申请人： Lung-Hu Wang ,  George Schloemer ,  Allen Liu

    发明人： Lung-Hu Wang ,  George Schloemer ,  Allen Liu

    IPC分类号： C07H19/048 ,  C07H19/12 ,  C07H19/00 ,  C07H19/22

    CPC分类号： C07H19/00 ,  C07H19/048 ,  C07H19/073 ,  C07H19/12 ,  C07H19/22 ,  Y02P20/55

    摘要： A process of preparing an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate, which is useful as an intermediate in the preparation of a beta nucleoside, such as gemcitabine, an anti-tumor agent. A beta-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate is heated and converted to an alpha-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate in the absence of an effective amount of a sulfonate salt to facilitate the conversion. In addition, an anomeric mixture of an alpha-anomer and a beta-anomer of 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate can be dissolved in a mixture of water and a solvent and heated to produce a lactol, which may be further converted to an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate.

    摘要翻译： 制备富含α-脱水异构体的2-脱氧-2,2-二氟-D-核糖核酸磺酸的方法，其可用作制备β核苷的中间体，例如吉西他滨，抗肿瘤剂。 在不存在有效量的磺酸盐的情况下，将β-2-脱氧-2,2-二氟-D-核糖核酸磺酸酯加热并转化成α-2-脱氧-2,2-二氟-D-核糖核酸磺酰基磺酸盐 以方便转换。 此外，可以将2-脱氧-2,2-二氟-D-核糖核酸磺酸的α-端基异构体和β-端基异头体的端基异构体混合物溶解在水和溶剂的混合物中，并加热产生内酯， 可进一步转化为富含α-脱水异构体的2-脱氧-2,2-二氟-D-核糖核酸磺酰基磺酸酯。

    Crystalline form of ivacaftor and a process for preparing the same
    25.
    发明授权
    Crystalline form of ivacaftor and a process for preparing the same 有权

    公开(公告)号：US11384054B2

    公开(公告)日：2022-07-12

    申请号：US17200132

    申请日：2021-03-12

    申请人： ScinoPharm Taiwan, Ltd.

    发明人： Kuan-Hsun Huang ,  Li-Ting Wang ,  Inze Lin ,  Tsung-Cheng Hu

    IPC分类号： C07D215/56

    摘要： In certain aspects, the invention provides crystalline forms of ivacaftor N-(2,4-di-tert-butyl-phenyl-5-hydroxy-phenyl)-1,4-dihydro-4-oxoquinoline-3-carboxamide. In related aspects, the invention provides a process for preparing any one of crystalline forms S2, S3, S4 and S5 of ivacaftor. The process includes: forming a solution including crude ivacaftor and a solvent; adding an anti-solvent to the solution to form slurry including a precipitate; isolating the precipitate; and drying the precipitate to provide crystalline form S2, S3, S4, or S5 of ivacaftor.

    PROCESS FOR PREPARING OSIMERTINIB OR A SALT THEREOF
    26.
    发明申请
    PROCESS FOR PREPARING OSIMERTINIB OR A SALT THEREOF 有权

    公开(公告)号：US20220185794A1

    公开(公告)日：2022-06-16

    申请号：US17123556

    申请日：2020-12-16

    申请人： ScinoPharm Taiwan, Ltd.

    发明人： Kuan-Hsun Huang ,  Chung-Yang Huang ,  Tsung-Cheng Hu

    IPC分类号： C07D403/04 ,  B01J23/44 ,  C07C309/04

    摘要： Provided herein are improved processes and methods for preparing osimertinib or a salt thereof, in particular osimertinib mesylate. The improved process removes the necessity of isolating the unstable aniline intermediate of formula (III) and enables the direct coupling to form the amide product of formula (II): The present invention is suitable for a large-scale production, avoiding the isolation of unstable intermediate, thereby providing osimertinib or a mesylate salt thereof in both high yields and high purity.

    Polymorphism for irinotecan free base
    27.
    发明授权
    Polymorphism for irinotecan free base 有权

    公开(公告)号：US10919905B2

    公开(公告)日：2021-02-16

    申请号：US16830561

    申请日：2020-03-26

    申请人： ScinoPharm Taiwan, Ltd.

    发明人： Yuan-Xiu Liao ,  Yuan-Chang Huang

    IPC分类号： C07D491/22

    摘要： Crystalline form S1 of irinotecan free base characterized by a powder X-ray diffraction pattern with peaks at about 8.7±0.2, 13.1±0.2, 14.5±0.2, 17.4±0.2, 18.4±0.2, 20.9±0.2, 24.0±0.2 and 27.5±0.2 degrees two-theta degrees two-theta, and crystalline form S2 of irinotecan free base characterized by a powder X-ray diffraction pattern with peaks at about 7.1±0.2, 10.6±0.2, 12.4±0.2, 20.6±0.2, 21.6±0.2 and 24.2±0.2 degrees two-theta.

    Process for preparing lifitegrast and intermediates thereof
    29.
    发明授权
    Process for preparing lifitegrast and intermediates thereof 有权

    公开(公告)号：US10428052B2

    公开(公告)日：2019-10-01

    申请号：US16023580

    申请日：2018-06-29

    申请人： ScinoPharm Taiwan, Ltd.

    发明人： Ming-Chih Wu ,  Tsung-Yu Hsiao

    IPC分类号： C07D405/06 ,  C07D405/12

    摘要： The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.