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    • 68. 发明公开
    • PROCESS FOR THE PRODUCTION OF MYCOPHENOLATE MOFETIL
    • 生产霉酚酸酯的方法MOFETIL
    • EP1667987A2
    • 2006-06-14
    • EP04765061.9
    • 2004-09-10
    • SANDOZ AG
    • GREIL, JuliaLUDESCHER, JohannesWOLF, Siegfried
    • C07D307/88
    • C07D307/88
    • The present invention relates to a new and economically attractive process for the production of mycophenolate mofetil in a high degree of pharmaceutically acceptable purity, which comprises the reaction of a reactive derivative of mycophenolic acid with 4-(2-hydroxyethyl)morpholine under acidic reaction conditions and the subsequent extraction of the pure mycophenolate mofetil through salt formation and release of the free base. A further aspect of the invention relates to the purification of mycophenolate mofetil by removing its by products, in particular its dimeric by-products, by means of treatment with a primary or secondary amine.
    • 本发明涉及一种以高度药学上可接受的纯度生产霉酚酸吗啉乙酯的新的且经济上有吸引力的方法,其包括霉酚酸的反应性衍生物与4-(2-羟乙基)吗啉在酸性反应条件下反应 并随后通过盐形成和游离碱的释放来提取纯麦考酚酸吗乙酯。 本发明的另一方面涉及通过用伯胺或仲胺处理除去其副产物,特别是其二聚副产物来纯化麦考酚酸吗啉乙酯。