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    PROCESS FOR THE PREPARATION OF IOPAMIDOL
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF IOPAMIDOL 审中-公开

    公开(公告)号：EP3369724A1

    公开(公告)日：2018-09-05

    申请号：EP18162482.6

    申请日：2014-11-04

    申请人： Bracco Imaging SPA

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

    IPC分类号： C07C231/02 ,  C07F5/02 ,  C07F5/04

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

    摘要： The present invention discloses a process for the preparation of lopamidol of formula (II)

    and comprising the following steps:
    a) reacting the Compound (I) wherein X is OR 2 or R 3 , and wherein R 2 and R 3 are a C 1 -C 6 linear or branched alkyl, C 3 -C 6 cycloalkyl, C 6 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 hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain lopamidol (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.