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    PREPARATION OF A SOLID FORM OF GADOBENATE DIMEGLUMINE
    101.
    发明申请
    PREPARATION OF A SOLID FORM OF GADOBENATE DIMEGLUMINE 审中-公开

    公开(公告)号：US20200071341A1

    公开(公告)日：2020-03-05

    申请号：US16678082

    申请日：2019-11-08

    申请人： BRACCO IMAGING S.P.A.

    发明人： Roberta MAZZON ,  Roberta FRETTA ,  Pier Lucio ANELLI

    IPC分类号： C07F5/00 ,  A61K49/18 ,  A61K49/10 ,  C07C227/40 ,  A61K9/00 ,  A61K9/14

    摘要： The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.

    PROCESS FOR THE PREPARATION OF IOPAMIDOL
    102.
    发明申请
    PROCESS FOR THE PREPARATION OF IOPAMIDOL 审中-公开

    公开(公告)号：US20190071392A1

    公开(公告)日：2019-03-07

    申请号：US15912772

    申请日：2018-03-06

    申请人： BRACCO IMAGING S.P.A.

    发明人： Elisa BATTISTINI ,  Federica BUONSANTI ,  Daniela IMPERIO ,  Luciano LATTUADA ,  Roberta NAPOLITANO

    IPC分类号： C07C231/14 ,  C07F5/02 ,  C07C231/12 ,  C07C227/04 ,  C07C201/12 ,  C07C231/02 ,  C07F5/05 ,  C07F5/04 ,  C07C237/46

    CPC分类号： C07C231/14 ,  C07C201/12 ,  C07C227/04 ,  C07C231/02 ,  C07C231/12 ,  C07C237/46 ,  C07F5/025 ,  C07F5/04 ,  C07F5/05 ,  Y02P20/55 ,  Y02P20/582

    摘要： The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N—(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline N hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness.

    Process for the preparation of chelated compounds
    107.
    发明授权
    Process for the preparation of chelated compounds 有权
    螯合化合物的制备方法

    公开(公告)号：US09567350B2

    公开(公告)日：2017-02-14

    申请号：US14623202

    申请日：2015-02-16

    申请人： BRACCO IMAGING S.P.A.

    发明人： Federico Maisano ,  Federico Crivellin

    IPC分类号： C07F5/00 ,  C07C227/16 ,  C07C227/40

    CPC分类号： C07F5/003 ,  C07C227/16 ,  C07C227/40 ,  C07C229/76

    摘要： The present invention generally relies on a process for the preparation of chelated compounds, comprising the selective interaction between a solid matrix and a chelating agent. In more details, the present invention enables the preparation of chelated compounds useful as diagnostic agents, in high yields and in a reliable way.

    摘要翻译： 本发明通常依赖于制备螯合化合物的方法，其包括固体基质和螯合剂之间的选择性相互作用。 更详细地说，本发明能够以高产率和可靠的方式制备用作诊断剂的螯合化合物。