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    • 6. 发明申请
    • METHOD FOR PREPARING ARGATROBAN MONOHYDRATE
    • 制备阿糖胞苷单硬脂酸酯的方法
    • WO2009124906A2
    • 2009-10-15
    • PCT/EP2009054085
    • 2009-04-06
    • LUNDBECK PHARMACEUTICALS ITALYZANON JACOPOLIBRALON GIOVANNANICOLE ANDREA
    • ZANON JACOPOLIBRALON GIOVANNANICOLE ANDREA
    • C07D401/12
    • C07D401/12
    • A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2- piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico- chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.
    • 描述了从(2R,4R)-1- [NG-硝基-N 2 - (3-甲基-8-喹啉磺酰基)-L-精氨酰基] -4-甲基-2-哌啶羧酸得到的制备阿格曲班一水合物的方法, 适当处理粗制阿加曲班。 该方法包括在连续步骤中制备阿加曲班一水合物或分离纯化的阿加曲班的中间步骤。 也可从阿加曲班一水合物获得的是无水阿加曲班,显示具有新的物理化学特性。 所述的阿加曲班合成和纯化方法因此能够获得三种不同形式的阿加曲班,没有以前描述,其具有独特的物理化学特性,特别是能够以高产率和高纯度获得阿格曲班一水合物,因此是一种 适用于专利药物活性成分的产品。