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发明公开
CN107445858A 三碘化造影剂的生产 无效 - 撤回

三碘化造影剂的生产
摘要：
本发明涉及三碘化造影剂的生产。本发明还涉及一种新化合物，其为(S)-5-(2-乙酰氧基丙酰氨基)-2,4,6-三碘间苯二甲酸，具有式II(S)-5-(2-乙酰氧基丙酰氨基)-2,4,6-三碘间苯二甲酸。所述新化合物具有用于生产具有低含量的乙酰基和羟基乙酰基类似物的三碘化造影剂(尤其是碘帕醇)的用途。该新化合物可由5-氨基-2,4,6-三碘间苯二甲酸通过被(S)-1-氯-1-氧代丙-2-基乙酸酯酰化而形成。然后，可通过与氯化试剂反应将该新化合物转化为相应的酸二氯化物，之后用2-氨基-1,3-丙二醇进行酰胺化以及进行乙酸酯水解，所述酸二氯化物是本发明的另一个目的。(S)-5-(2-乙酰氧基丙酰氨基)-2,4,6-三碘间苯二甲酸。
摘要（英）：

The invention relates to manufacture of a triiodinated contrast agent. The invention further relates to a new compound, (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid, of formula II (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid. Said new compound is of use for the production of triiodinated contrast agent, especially lopamidol, with low content of acetyl and hydroxyacetyl analogs. The new compound may be formed from 5-amino-2,4,6-triiodoisophtalic acid by acylating with (S)-1-chloro-1-oxopropan-2-yl acetate. The new compound may then be converted to the respective acid dichloride by reacting with a chlorinating reagent, which is a further object of the present invention, followed by the amidation with 2-amino-1,3-propanediol and acetate hydrolysis.

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