Preparation of intermediates of X-ray contrast agents
    1.
    发明授权
    Preparation of intermediates of X-ray contrast agents 有权
    X射线造影剂中间体的制备

    公开(公告)号:US09403757B2

    公开(公告)日:2016-08-02

    申请号:US14437430

    申请日:2013-10-24

    申请人: GE Healthcare AS

    发明人: Torfinn Haaland

    摘要: The present invention relates to a process for the preparation of iodinated X-ray contrast agents and in particular to key intermediates thereof. It particularly relates to an improved process for preparation of 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (Compound A) or N,N′-bis(2,3-dihydroxypropyl)-5-formamido-2,4,6-triiodoisophthalamide (Compound C), which are intermediates in the industrial preparation of non-ionic X-ray contrast agents. More particularly the invention provides a process for deacylation of the acylated hydroxyl groups of an intermediate compound of Compound A and Compound C.

    摘要翻译: 本发明涉及一种制备碘化X射线造影剂的方法,特别涉及其关键中间体。 它特别涉及制备5-乙酰氨基-N,N'-双(2,3-二羟基丙基)-2,4,6-三碘间苯二酰胺(化合物A)或N,N'-双(2,3 - 二羟丙基)-5-甲酰氨基-2,4,6-三碘间苯二酰胺(化合物C),它们是非离子X射线造影剂的工业制备中的中间体。 更具体地,本发明提供了化合物A和化合物C的中间体化合物的酰化羟基脱酰基的方法。

    PREPARATION OF INTERMEDIATES OF X-RAY CONTRAST AGENTS
    4.
    发明申请
    PREPARATION OF INTERMEDIATES OF X-RAY CONTRAST AGENTS 有权
    X射线对比剂中间体的制备

    公开(公告)号:US20150274645A1

    公开(公告)日:2015-10-01

    申请号:US14437430

    申请日:2013-10-24

    申请人: GE Healthcare AS

    发明人: Torfinn Haaland

    摘要: The present invention relates to a process for the preparation of iodinated X-ray contrast agents and in particular to key intermediates thereof. It particularly relates to an improved process for preparation of 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (Compound A) or N,N′-bis(2,3-dihydroxypropyl)-5-formamido-2,4,6-triiodoisophthalamide (Compound C), which are intermediates in the industrial preparation of non-ionic X-ray contrast agents. More particularly the invention provides a process for deacylation of the acylated hydroxyl groups of an intermediate compound of Compound A and Compound C.

    摘要翻译: 本发明涉及一种制备碘化X射线造影剂的方法,特别涉及其关键中间体。 它特别涉及制备5-乙酰氨基-N,N'-双(2,3-二羟基丙基)-2,4,6-三碘间苯二酰胺(化合物A)或N,N'-双(2,3 - 二羟丙基)-5-甲酰氨基-2,4,6-三碘间苯二酰胺(化合物C),它们是非离子X射线造影剂的工业制备中的中间体。 更具体地,本发明提供了化合物A和化合物C的中间体化合物的酰化羟基脱酰基的方法。

    ALTERNATIVE ACETYLATION PROCESS IN THE SYNTHESIS OF NON-IONIC X-RAY CONTRAST AGENTS
    6.
    发明申请
    ALTERNATIVE ACETYLATION PROCESS IN THE SYNTHESIS OF NON-IONIC X-RAY CONTRAST AGENTS 有权
    非离子X射线对比剂合成中的替代乙酰化方法

    公开(公告)号:US20160304438A1

    公开(公告)日:2016-10-20

    申请号:US15100683

    申请日:2014-12-08

    申请人: GE HEALTHCARE AS

    IPC分类号: C07C231/02

    CPC分类号: C07C231/02 C07C237/46

    摘要: An alternative acetylation process for the synthesis of 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents, is described. The process can be performed on an industrial scale to produce Compound A with improved purity and improved yields compared to the established processes.

    摘要翻译: 用于合成5-乙酰氨基-N,N'-双(2,3-二羟丙基)-2,4,6-三碘间苯二酰胺(“化合物A”)的替代乙酰化方法,其是非离子型工业制备中的中间体 描述了X射线造影剂。 与已建立的方法相比,该方法可以在工业规模上进行以产生具有改进的纯度和提高的产率的化合物A.

    CONTINUOUS CRYSTALLISATION METHOD

    公开(公告)号:US20230133715A1

    公开(公告)日:2023-05-04

    申请号:US17912646

    申请日:2021-03-31

    申请人: GE Healthcare AS

    IPC分类号: C07C231/24 C07C237/46

    摘要: The invention provides a method of purifying 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide, comprising adding a portion of acid to a stream comprising crude 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide in a solvent and continuously crystallising the 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide from the crude 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide, with removal of at least a fraction of the solvent, wherein the crystallisation is carried out in a continuous reactor, wherein the continuous reactor is a plug flow reactor. At least three further portions of acid are added to the continuous reactor during the crystallisation.