IMPROVED FLUORINATION PROCESS
    1.
    发明申请
    IMPROVED FLUORINATION PROCESS 审中-公开
    改进的荧光过程

    公开(公告)号:WO2016066283A1

    公开(公告)日:2016-05-06

    申请号:PCT/EP2015/063999

    申请日:2015-06-22

    申请人: SANDOZ AG

    CPC分类号: C07H19/06 C07H1/00 C07H19/10

    摘要: A process comprising (i) providing a mixture comprising a compound of formula (I) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof; (ii)subjecting the mixture provided in (i) to fluorinating conditions in the presence of a fluorination agent selected from the group consisting of diethylamino (difluoro) sulfonium tetrafluoroborate and difluoro(morpholino) sulfonium tetrafluoroborate obtaining a mixture comprising a compound of formula (II) or isomers, stereoisomers diastereomers, enantiomers or salts thereof; (iii) optionally subjecting the mixture obtained in (ii) to deprotection conditions, obtaining a mixture comprising the compound of formula (III) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof.

    摘要翻译: 一种方法,包括(i)提供包含式(I)化合物或其异构体,立体异构体,非对映异构体,对映异构体或其盐的混合物; (ii)在选自二氟氨基(二氟)锍四氟硼酸二氟甲酯和二氟(吗啉代)锍四氟硼酸盐的氟化剂存在下,使(ⅰ)中提供的混合物经受氟化条件,得到包含式(II)化合物 )或异构体,立体异构体非对映异构体,对映异构体或其盐; (iii)任选地使(ii)中获得的混合物经脱保护条件,得到包含式(III)化合物或其异构体的混合物,立体异构体,非对映异构体,对映异构体或其盐。

    PROCESS FOR PRODUCING STERILE SOLUTIONS CONTAINING A CELLULOSE ETHER DERIVATIVE
    3.
    发明申请
    PROCESS FOR PRODUCING STERILE SOLUTIONS CONTAINING A CELLULOSE ETHER DERIVATIVE 审中-公开
    生产含有纤维素醚衍生物的固体溶液的方法

    公开(公告)号:WO2016097240A1

    公开(公告)日:2016-06-23

    申请号:PCT/EP2015/080390

    申请日:2015-12-18

    申请人: SANDOZ AG

    IPC分类号: A61K47/38 A61K9/00

    CPC分类号: A61K47/38 A61K9/0019

    摘要: The present invention relates to a process for producing a sterile solution containing a cellulose ether derivative, comprising the steps of i) providing a non-sterile solution containing a cellulose ether derivative, ii) sterile filtrating the solution of step i), and iii) removing the solvent under reduced pressure.

    摘要翻译: 本发明涉及一种生产含有纤维素醚衍生物的无菌溶液的方法,包括以下步骤:i)提供含有纤维素醚衍生物的非无菌溶液,ii)无菌过滤步骤i)的溶液,和iii) 减压除去溶剂。

    SYNTHESIS OF PHOSPHORAMIDATES
    5.
    发明申请
    SYNTHESIS OF PHOSPHORAMIDATES 审中-公开
    合成磷酸酯

    公开(公告)号:WO2016207194A1

    公开(公告)日:2016-12-29

    申请号:PCT/EP2016/064370

    申请日:2016-06-22

    申请人: SANDOZ AG

    IPC分类号: C07F9/6558

    CPC分类号: C07F9/65586 Y02P20/55

    摘要: A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).

    摘要翻译: 一种制备式(I)化合物或其盐的方法,该方法包括提供其中PG是惰性吸电子羟基保护基的式(III)化合物,使式(III)化合物与氟化剂 得到式(Ⅱ)化合物,并使式(Ⅱ)化合物脱保护。

    PROCESS FOR THE SYNTHESIS OF TELAPREVIR, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR SOLVATES AS WELL AS INTERMEDIATE PRODUCTS THEREOF
    8.
    发明申请
    PROCESS FOR THE SYNTHESIS OF TELAPREVIR, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR SOLVATES AS WELL AS INTERMEDIATE PRODUCTS THEREOF 审中-公开
    合成TELAPREVIR或药物可接受的盐或溶剂作为其中间产物的方法

    公开(公告)号:WO2013135870A1

    公开(公告)日:2013-09-19

    申请号:PCT/EP2013/055397

    申请日:2013-03-15

    申请人: SANDOZ AG

    IPC分类号: C07D403/12

    摘要: The invention relates to a process for the preparation of telaprevir, or a pharmaceutically acceptable salt or solvate thereof, wherein the process requires a smaller number of process steps and/or does not require the use of toxic and instable compounds compared to the known processes. Another embodiment refers to telaprevir, or a pharmaceutically acceptable salt or solvate thereof as well as to intermediate products for preparation of the same, wherein the afore-mentioned products are obtained by the process described herein.

    摘要翻译: 本发明涉及一种制备特拉匹韦或其药学上可接受的盐或溶剂合物的方法,其中与已知方法相比,该方法需要较少数量的工艺步骤和/或不需要使用有毒和不稳定的化合物。 另一个实施方案是指特拉匹韦或其药学上可接受的盐或溶剂化物以及用于制备其的中间产物,其中上述产物通过本文所述的方法获得。

    SYNTHESIS OF PHOSPHORAMIDATES
    9.
    发明申请

    公开(公告)号:WO2018134343A1

    公开(公告)日:2018-07-26

    申请号:PCT/EP2018/051286

    申请日:2018-01-19

    申请人: SANDOZ AG

    IPC分类号: C07H1/00 C07H19/10

    CPC分类号: C07H1/00 C07H19/10

    摘要: The present invention is directed to a compound of formula (III), its preparation and to its use for the preparation of a compound of formula (IV). The present invention hence is directed to a process for the preparation of compound of formula (III) and for the preparation of a compound of formula (IV) from a compound of formula (III) via reduction of the compound of formula (III). The present invention is further directed to intermediate compounds for preparing the compound of formula (III) and hence compound of formula (IV).