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    CONTINUOUS PROCESS FOR THE PREPARATION OF (S)-2-ACETYLOXYPROPIONIC ACID CHLORIDE
    1.
    发明公开
    CONTINUOUS PROCESS FOR THE PREPARATION OF (S)-2-ACETYLOXYPROPIONIC ACID CHLORIDE 有权
    （S）-2-乙酰氧基丙酸氯化物的连续制备方法

    公开(公告)号：EP2931696A1

    公开(公告)日：2015-10-21

    申请号：EP13801552.4

    申请日：2013-12-04

    申请人： Bracco Imaging S.p.A

    发明人： CERAGIOLI, Silvia ,  DELOGU, Pietro ,  MORTILLARO, Armando ,  NARDELLI, Alfonso ,  SGUASSERO, Stefano ,  VELARDI, Rosario ,  VISCARDI, Carlo Felice

    IPC分类号： C07C67/08 ,  C07C69/22

    CPC分类号： C07C67/313 ,  C07C67/08 ,  C07C67/287 ,  C07C71/00 ,  Y02P20/582 ,  C07C69/14

    摘要： The present invention relates to a continuous method for the preparation of (S)-2-acetyloxypropionic acid from an aqueous solution of lactic acid and acetic anhydride, in acetic acid. (S)-2-acetyloxypropionic acid is used for the preparation of (S)-2-acetyloxypropionic acid chloride, an essential intermediate compound for the preparation of lopamidol and has to be industrially produced with high purity and suitable quality for producing lopamidol according to the Pharmacopoeia requirements. The continuous process according to the invention, comprises therefore also the chlorination steps of (S)-2-acetyloxypropionic acid with thionyl chloride to give the corresponding (S)-2-acetyloxypropionic acid chloride which is further distilled to give the suitable purity characteristics for its use for the preparation of non-ionic iodinated contrast agents as lopamidol.

    摘要翻译： 本发明涉及由乳酸和乙酸酐的水溶液在乙酸中制备（S）-2-乙酰氧基丙酸的连续方法。 （S）-2-乙酰氧基丙酸用于制备用于制备碘帕醇的必需中间体化合物（S）-2-乙酰氧基丙酰氯，并且必须在工业上生产具有高纯度和合适品质的用于生产碘帕醇的根据 药典要求。 因此，根据本发明的连续方法还包括（S）-2-乙酰氧基丙酸与亚硫酰氯的氯化步骤以得到相应的（S）-2-乙酰氧基丙酰氯，其被进一步蒸馏以给出合适的纯度特性 其用于制备非离子型碘化造影剂如碘帕醇。